Details of the Target
General Information of Target
Target ID | LDTP10809 | |||||
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Target Name | SRSF protein kinase 1 (SRPK1) | |||||
Gene Name | SRPK1 | |||||
Gene ID | 6732 | |||||
Synonyms |
SRSF protein kinase 1; EC 2.7.11.1; SFRS protein kinase 1; Serine/arginine-rich protein-specific kinase 1; SR-protein-specific kinase 1 |
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3D Structure | ||||||
Sequence |
MMKTEPRGPGGPLRSASPHRSAYEAGIQALKPPDAPGPDEAPKGAHHKKYGSNVHRIKSM
FLQMGTTAGPSGEAGGGAGLAEAPRASERGVRLSLPRASSLNENVDHSALLKLGTSVSER VSRFDSKPAPSAQPAPPPHPPSRLQETRKLFERSAPAAAGGDKEAAARRLLRQERAGLQD RKLDVVVRFNGSTEALDKLDADAVSPTVSQLSAVFEKADSRTGLHRGPGLPRAAGVPQVN SKLVSKRSRVFQPPPPPPPAPSGDAPAEKERCPAGQQPPQHRVAPARPPPKPREVRKIKP VEVEESGESEAESAPGEVIQAEVTVHAALENGSTVATAASPAPEEPKAQAAPEKEAAAVA PPERGVGNGRAPDVAPEEVDESKKEDFSEADLVDVSAYSGLGEDSAGSALEEDDEDDEED GEPPYEPESGCVEIPGLSEEEDPAPSRKIHFSTAPIQVFSTYSNEDYDRRNEDVDPMAAS AEYELEKRVERLELFPVELEKDSEGLGISIIGMGAGADMGLEKLGIFVKTVTEGGAAHRD GRIQVNDLLVEVDGTSLVGVTQSFAASVLRNTKGRVRFMIGRERPGEQSEVAQLIQQTLE QERWQREMMEQRYAQYGEDDEETGEYATDEDEELSPTFPGGEMAIEVFELAENEDALSPV DMEPEKLVHKFKELQIKHAVTEAEIQQLKRKLQSLEQEKGRWRVEKAQLEQSVEENKERM EKLEGYWGEAQSLCQAVDEHLRETQAQYQALERKYSKAKRLIKDYQQKEIEFLKKETAQR RVLEESELARKEEMDKLLDKISELEGNLQTLRNSNST |
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Target Type |
Preclinical
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Target Bioclass |
Enzyme
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Family |
Protein kinase superfamily, CMGC Ser/Thr protein kinase family
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Subcellular location |
Cytoplasm
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Function |
Serine/arginine-rich protein-specific kinase which specifically phosphorylates its substrates at serine residues located in regions rich in arginine/serine dipeptides, known as RS domains and is involved in the phosphorylation of SR splicing factors and the regulation of splicing. Plays a central role in the regulatory network for splicing, controlling the intranuclear distribution of splicing factors in interphase cells and the reorganization of nuclear speckles during mitosis. Can influence additional steps of mRNA maturation, as well as other cellular activities, such as chromatin reorganization in somatic and sperm cells and cell cycle progression. Isoform 2 phosphorylates SFRS2, ZRSR2, LBR and PRM1. Isoform 2 phosphorylates SRSF1 using a directional (C-terminal to N-terminal) and a dual-track mechanism incorporating both processive phosphorylation (in which the kinase stays attached to the substrate after each round of phosphorylation) and distributive phosphorylation steps (in which the kinase and substrate dissociate after each phosphorylation event). The RS domain of SRSF1 binds first to a docking groove in the large lobe of the kinase domain of SRPK1. This induces certain structural changes in SRPK1 and/or RRM2 domain of SRSF1, allowing RRM2 to bind the kinase and initiate phosphorylation. The cycles continue for several phosphorylation steps in a processive manner (steps 1-8) until the last few phosphorylation steps (approximately steps 9-12). During that time, a mechanical stress induces the unfolding of the beta-4 motif in RRM2, which then docks at the docking groove of SRPK1. This also signals RRM2 to begin to dissociate, which facilitates SRSF1 dissociation after phosphorylation is completed. Isoform 2 can mediate hepatitis B virus (HBV) core protein phosphorylation. It plays a negative role in the regulation of HBV replication through a mechanism not involving the phosphorylation of the core protein but by reducing the packaging efficiency of the pregenomic RNA (pgRNA) without affecting the formation of the viral core particles. Isoform 1 and isoform 2 can induce splicing of exon 10 in MAPT/TAU. The ratio of isoform 1/isoform 2 plays a decisive role in determining cell fate in K-562 leukaemic cell line: isoform 2 favors proliferation where as isoform 1 favors differentiation.
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TTD ID | ||||||
Uniprot ID | ||||||
DrugMap ID | ||||||
Ensemble ID | ||||||
HGNC ID | ||||||
ChEMBL ID |
Probe(s) Labeling This Target
ABPP Probe
Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
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m-APA Probe Info |
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15.00 | LDD0402 | [1] | |
STPyne Probe Info |
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K25(6.67); K4(10.00); K486(0.97); K579(10.00) | LDD0277 | [2] | |
Probe 1 Probe Info |
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Y117(14.40) | LDD3495 | [3] | |
DBIA Probe Info |
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C359(3.35) | LDD3312 | [4] | |
BTD Probe Info |
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C188(0.50) | LDD2089 | [5] | |
DA-P3 Probe Info |
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5.05 | LDD0182 | [6] | |
AHL-Pu-1 Probe Info |
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C502(2.14); C455(2.02) | LDD0168 | [7] | |
ATP probe Probe Info |
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K506(0.00); K215(0.00); K191(0.00) | LDD0199 | [8] | |
4-Iodoacetamidophenylacetylene Probe Info |
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C455(0.00); C647(0.00); C188(0.00); C502(0.00) | LDD0038 | [9] | |
IA-alkyne Probe Info |
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N.A. | LDD0032 | [10] | |
IPIAA_L Probe Info |
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N.A. | LDD0031 | [11] | |
Lodoacetamide azide Probe Info |
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C455(0.00); C647(0.00); C502(0.00); C188(0.00) | LDD0037 | [9] | |
NAIA_4 Probe Info |
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C356(0.00); C455(0.00) | LDD2226 | [12] | |
WYneO Probe Info |
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N.A. | LDD0022 | [13] | |
Compound 10 Probe Info |
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C502(0.00); C647(0.00) | LDD2216 | [14] | |
ENE Probe Info |
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N.A. | LDD0006 | [13] | |
IPM Probe Info |
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C356(0.00); C455(0.00); C647(0.00) | LDD0147 | [15] | |
PF-06672131 Probe Info |
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N.A. | LDD0017 | [16] | |
SF Probe Info |
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N.A. | LDD0028 | [17] | |
TFBX Probe Info |
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C188(0.00); C455(0.00) | LDD0148 | [15] | |
VSF Probe Info |
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N.A. | LDD0007 | [13] | |
Acrolein Probe Info |
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C455(0.00); C647(0.00); C188(0.00) | LDD0217 | [18] | |
Crotonaldehyde Probe Info |
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C647(0.00); C455(0.00) | LDD0219 | [18] | |
Methacrolein Probe Info |
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C455(0.00); C647(0.00) | LDD0218 | [18] | |
W1 Probe Info |
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N.A. | LDD0236 | [19] | |
AOyne Probe Info |
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15.00 | LDD0443 | [20] | |
NAIA_5 Probe Info |
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C455(0.00); C647(0.00) | LDD2223 | [12] |
PAL-AfBPP Probe
Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
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C056 Probe Info |
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16.56 | LDD1753 | [21] | |
FFF probe14 Probe Info |
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20.00 | LDD0477 | [22] | |
FFF probe2 Probe Info |
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5.86 | LDD0463 | [22] | |
Probe 12 Probe Info |
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N.A. | LDD0420 | [23] |
Competitor(s) Related to This Target
Competitor ID | Name | Cell line | Binding Site(Ratio) | Interaction ID | Ref |
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LDCM0502 | 1-(Cyanoacetyl)piperidine | MDA-MB-231 | C188(0.55) | LDD2095 | [5] |
LDCM0537 | 2-Cyano-N,N-dimethylacetamide | MDA-MB-231 | C188(0.93) | LDD2130 | [5] |
LDCM0524 | 2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide | MDA-MB-231 | C188(0.97); C455(1.21) | LDD2117 | [5] |
LDCM0558 | 2-Cyano-N-phenylacetamide | MDA-MB-231 | C188(1.59) | LDD2152 | [5] |
LDCM0538 | 4-(Cyanoacetyl)morpholine | MDA-MB-231 | C188(0.81) | LDD2131 | [5] |
LDCM0025 | 4SU-RNA | HEK-293T | C502(2.14); C455(2.02) | LDD0168 | [7] |
LDCM0026 | 4SU-RNA+native RNA | DM93 | C455(5.75); C356(8.12) | LDD0171 | [7] |
LDCM0214 | AC1 | HEK-293T | C647(0.97); C455(1.04); C356(0.91) | LDD1507 | [24] |
LDCM0215 | AC10 | HEK-293T | C647(1.02); C455(0.94); C356(1.04) | LDD1508 | [24] |
LDCM0226 | AC11 | HEK-293T | C647(0.98); C455(0.95); C188(0.92); C356(0.97) | LDD1509 | [24] |
LDCM0237 | AC12 | HEK-293T | C455(0.92); C356(1.11) | LDD1510 | [24] |
LDCM0259 | AC14 | HEK-293T | C647(1.00); C455(0.99); C356(1.04) | LDD1512 | [24] |
LDCM0270 | AC15 | HEK-293T | C647(0.99); C455(1.06); C188(0.93) | LDD1513 | [24] |
LDCM0276 | AC17 | HEK-293T | C647(0.94); C455(0.98); C356(1.00) | LDD1515 | [24] |
LDCM0277 | AC18 | HEK-293T | C647(1.06); C455(0.99); C356(1.04) | LDD1516 | [24] |
LDCM0278 | AC19 | HEK-293T | C647(1.05); C455(1.02); C188(0.82); C356(1.13) | LDD1517 | [24] |
LDCM0279 | AC2 | HEK-293T | C647(1.01); C455(0.97); C356(1.11) | LDD1518 | [24] |
LDCM0280 | AC20 | HEK-293T | C455(0.98); C356(1.09) | LDD1519 | [24] |
LDCM0281 | AC21 | HEK-293T | C647(1.04); C455(1.05); C188(1.05); C356(0.95) | LDD1520 | [24] |
LDCM0282 | AC22 | HEK-293T | C647(0.93); C455(0.98); C356(1.10) | LDD1521 | [24] |
LDCM0283 | AC23 | HEK-293T | C647(0.93); C455(0.95); C188(1.08) | LDD1522 | [24] |
LDCM0284 | AC24 | HEK-293T | C647(1.00); C455(1.02); C356(0.89) | LDD1523 | [24] |
LDCM0285 | AC25 | HEK-293T | C647(0.96); C455(1.00); C356(0.99) | LDD1524 | [24] |
LDCM0286 | AC26 | HEK-293T | C647(1.03); C455(0.99); C356(1.05) | LDD1525 | [24] |
LDCM0287 | AC27 | HEK-293T | C647(1.13); C455(0.94); C188(0.92); C356(1.01) | LDD1526 | [24] |
LDCM0288 | AC28 | HEK-293T | C455(0.95); C356(1.14) | LDD1527 | [24] |
LDCM0289 | AC29 | HEK-293T | C647(1.01); C455(1.05); C188(0.98); C356(0.97) | LDD1528 | [24] |
LDCM0290 | AC3 | HEK-293T | C647(1.21); C455(0.95); C188(0.93); C356(1.24) | LDD1529 | [24] |
LDCM0291 | AC30 | HEK-293T | C647(1.02); C455(0.98); C356(0.99) | LDD1530 | [24] |
LDCM0292 | AC31 | HEK-293T | C647(1.00); C455(0.94); C188(1.09) | LDD1531 | [24] |
LDCM0293 | AC32 | HEK-293T | C647(0.99); C455(1.03); C356(0.97) | LDD1532 | [24] |
LDCM0294 | AC33 | HEK-293T | C647(0.96); C455(0.95); C356(0.99) | LDD1533 | [24] |
LDCM0295 | AC34 | HEK-293T | C647(0.96); C455(0.94); C356(1.24) | LDD1534 | [24] |
LDCM0296 | AC35 | HEK-293T | C647(1.11); C455(0.86); C188(0.93); C356(1.32) | LDD1535 | [24] |
LDCM0297 | AC36 | HEK-293T | C455(0.87); C356(1.13) | LDD1536 | [24] |
LDCM0298 | AC37 | HEK-293T | C647(1.06); C455(0.88); C188(1.06); C356(1.11) | LDD1537 | [24] |
LDCM0299 | AC38 | HEK-293T | C647(1.04); C455(1.03); C356(0.99) | LDD1538 | [24] |
LDCM0300 | AC39 | HEK-293T | C647(1.03); C455(1.07); C188(1.05) | LDD1539 | [24] |
LDCM0301 | AC4 | HEK-293T | C455(0.96); C356(1.14) | LDD1540 | [24] |
LDCM0302 | AC40 | HEK-293T | C647(1.01); C455(0.93); C356(0.98) | LDD1541 | [24] |
LDCM0303 | AC41 | HEK-293T | C647(0.98); C455(1.00); C356(0.99) | LDD1542 | [24] |
LDCM0304 | AC42 | HEK-293T | C647(1.01); C455(0.97); C356(1.42) | LDD1543 | [24] |
LDCM0305 | AC43 | HEK-293T | C647(1.09); C455(0.93); C188(0.97); C356(1.01) | LDD1544 | [24] |
LDCM0306 | AC44 | HEK-293T | C455(0.94); C356(0.99) | LDD1545 | [24] |
LDCM0307 | AC45 | HEK-293T | C647(1.10); C455(0.96); C188(1.05); C356(0.96) | LDD1546 | [24] |
LDCM0308 | AC46 | HEK-293T | C647(1.01); C455(0.97); C356(0.92) | LDD1547 | [24] |
LDCM0309 | AC47 | HEK-293T | C647(1.01); C455(1.08); C188(1.13) | LDD1548 | [24] |
LDCM0310 | AC48 | HEK-293T | C647(0.99); C455(1.02); C356(1.07) | LDD1549 | [24] |
LDCM0311 | AC49 | HEK-293T | C647(0.95); C455(0.95); C356(0.85) | LDD1550 | [24] |
LDCM0312 | AC5 | HEK-293T | C647(0.99); C455(0.93); C188(1.11); C356(1.05) | LDD1551 | [24] |
LDCM0313 | AC50 | HEK-293T | C647(1.01); C455(0.94); C356(1.25) | LDD1552 | [24] |
LDCM0314 | AC51 | HEK-293T | C647(1.06); C455(0.93); C188(0.96); C356(1.11) | LDD1553 | [24] |
LDCM0315 | AC52 | HEK-293T | C455(0.99); C356(1.10) | LDD1554 | [24] |
LDCM0316 | AC53 | HEK-293T | C647(1.04); C455(0.87); C188(1.05); C356(1.27) | LDD1555 | [24] |
LDCM0317 | AC54 | HEK-293T | C647(1.02); C455(1.00); C356(0.91) | LDD1556 | [24] |
LDCM0318 | AC55 | HEK-293T | C647(0.93); C455(1.02); C188(1.04) | LDD1557 | [24] |
LDCM0319 | AC56 | HEK-293T | C647(1.03); C455(0.97); C356(0.98) | LDD1558 | [24] |
LDCM0320 | AC57 | HEK-293T | C647(1.01); C455(0.93); C356(1.00) | LDD1559 | [24] |
LDCM0321 | AC58 | HEK-293T | C647(1.08); C455(0.96); C356(1.15) | LDD1560 | [24] |
LDCM0322 | AC59 | HEK-293T | C647(1.07); C455(0.92); C188(0.98); C356(1.00) | LDD1561 | [24] |
LDCM0323 | AC6 | HEK-293T | C647(0.96); C455(0.99); C356(1.11) | LDD1562 | [24] |
LDCM0324 | AC60 | HEK-293T | C455(0.93); C356(1.12) | LDD1563 | [24] |
LDCM0325 | AC61 | HEK-293T | C647(0.98); C455(0.93); C188(1.03); C356(0.99) | LDD1564 | [24] |
LDCM0326 | AC62 | HEK-293T | C647(1.01); C455(1.01); C356(1.05) | LDD1565 | [24] |
LDCM0327 | AC63 | HEK-293T | C647(0.98); C455(1.05); C188(0.96) | LDD1566 | [24] |
LDCM0328 | AC64 | HEK-293T | C647(1.07); C455(0.95); C356(1.03) | LDD1567 | [24] |
LDCM0334 | AC7 | HEK-293T | C647(1.01); C455(1.03); C188(1.16) | LDD1568 | [24] |
LDCM0345 | AC8 | HEK-293T | C647(0.94); C455(0.98); C356(1.07) | LDD1569 | [24] |
LDCM0545 | Acetamide | MDA-MB-231 | C188(0.38) | LDD2138 | [5] |
LDCM0520 | AKOS000195272 | MDA-MB-231 | C188(0.23) | LDD2113 | [5] |
LDCM0248 | AKOS034007472 | HEK-293T | C647(1.14); C455(0.95); C188(1.11); C356(0.95) | LDD1511 | [24] |
LDCM0356 | AKOS034007680 | HEK-293T | C647(0.91); C455(1.03); C356(0.83) | LDD1570 | [24] |
LDCM0275 | AKOS034007705 | HEK-293T | C647(1.01); C455(0.96); C356(0.97) | LDD1514 | [24] |
LDCM0156 | Aniline | NCI-H1299 | 11.71 | LDD0403 | [1] |
LDCM0498 | BS-3668 | MDA-MB-231 | C188(0.56); C455(0.65) | LDD2091 | [5] |
LDCM0108 | Chloroacetamide | HeLa | C455(0.00); C647(0.00) | LDD0222 | [18] |
LDCM0367 | CL1 | HEK-293T | C647(1.06); C455(0.95); C188(0.92); C356(1.32) | LDD1571 | [24] |
LDCM0368 | CL10 | HEK-293T | C647(1.01); C455(0.84); C356(1.11) | LDD1572 | [24] |
LDCM0369 | CL100 | HEK-293T | C647(1.01); C455(0.91); C188(0.94); C356(0.92) | LDD1573 | [24] |
LDCM0370 | CL101 | HEK-293T | C647(0.98); C455(0.93); C188(0.94); C356(1.15) | LDD1574 | [24] |
LDCM0371 | CL102 | HEK-293T | C647(1.01); C455(0.87); C356(1.13) | LDD1575 | [24] |
LDCM0372 | CL103 | HEK-293T | C647(0.99); C455(0.88); C188(1.00); C356(1.09) | LDD1576 | [24] |
LDCM0373 | CL104 | HEK-293T | C647(1.00); C455(0.86); C188(0.92); C356(1.13) | LDD1577 | [24] |
LDCM0374 | CL105 | HEK-293T | C647(0.94); C455(1.00); C188(1.04); C356(1.11) | LDD1578 | [24] |
LDCM0375 | CL106 | HEK-293T | C647(1.10); C455(0.89); C356(1.24) | LDD1579 | [24] |
LDCM0376 | CL107 | HEK-293T | C647(1.10); C455(0.92); C188(1.03); C356(1.05) | LDD1580 | [24] |
LDCM0377 | CL108 | HEK-293T | C647(1.01); C455(1.01); C188(0.93); C356(1.11) | LDD1581 | [24] |
LDCM0378 | CL109 | HEK-293T | C647(0.91); C455(0.96); C188(1.02); C356(1.15) | LDD1582 | [24] |
LDCM0379 | CL11 | HEK-293T | C647(1.05); C455(1.11); C188(1.51) | LDD1583 | [24] |
LDCM0380 | CL110 | HEK-293T | C647(1.01); C455(0.82); C356(1.06) | LDD1584 | [24] |
LDCM0381 | CL111 | HEK-293T | C647(1.03); C455(0.85); C188(0.98); C356(0.92) | LDD1585 | [24] |
LDCM0382 | CL112 | HEK-293T | C647(1.10); C455(0.99); C188(0.88); C356(1.17) | LDD1586 | [24] |
LDCM0383 | CL113 | HEK-293T | C647(1.00); C455(0.95); C188(0.91); C356(1.04) | LDD1587 | [24] |
LDCM0384 | CL114 | HEK-293T | C647(1.03); C455(0.77); C356(1.07) | LDD1588 | [24] |
LDCM0385 | CL115 | HEK-293T | C647(1.05); C455(0.87); C188(0.95); C356(1.09) | LDD1589 | [24] |
LDCM0386 | CL116 | HEK-293T | C647(1.12); C455(0.85); C188(0.89); C356(1.29) | LDD1590 | [24] |
LDCM0387 | CL117 | HEK-293T | C647(1.07); C455(0.99); C188(0.99); C356(1.09) | LDD1591 | [24] |
LDCM0388 | CL118 | HEK-293T | C647(1.05); C455(0.92); C356(1.38) | LDD1592 | [24] |
LDCM0389 | CL119 | HEK-293T | C647(1.03); C455(0.87); C188(1.06); C356(1.00) | LDD1593 | [24] |
LDCM0390 | CL12 | HEK-293T | C647(0.97); C455(0.96); C356(1.08) | LDD1594 | [24] |
LDCM0391 | CL120 | HEK-293T | C647(1.05); C455(0.90); C188(0.91); C356(1.07) | LDD1595 | [24] |
LDCM0392 | CL121 | HEK-293T | C647(1.00); C455(0.92); C188(0.99); C356(1.13) | LDD1596 | [24] |
LDCM0393 | CL122 | HEK-293T | C647(1.04); C455(0.95); C356(1.20) | LDD1597 | [24] |
LDCM0394 | CL123 | HEK-293T | C647(0.95); C455(0.85); C188(1.06); C356(1.04) | LDD1598 | [24] |
LDCM0395 | CL124 | HEK-293T | C647(1.00); C455(0.83); C188(1.03); C356(1.07) | LDD1599 | [24] |
LDCM0396 | CL125 | HEK-293T | C647(0.93); C455(1.00); C188(1.09); C356(1.34) | LDD1600 | [24] |
LDCM0397 | CL126 | HEK-293T | C647(1.02); C455(0.88); C356(1.10) | LDD1601 | [24] |
LDCM0398 | CL127 | HEK-293T | C647(1.11); C455(0.86); C188(1.04); C356(1.15) | LDD1602 | [24] |
LDCM0399 | CL128 | HEK-293T | C647(0.92); C455(0.90); C188(0.94); C356(1.13) | LDD1603 | [24] |
LDCM0400 | CL13 | HEK-293T | C647(0.86); C455(1.03); C188(0.88); C356(1.21) | LDD1604 | [24] |
LDCM0401 | CL14 | HEK-293T | C647(0.97); C455(0.88); C356(1.24) | LDD1605 | [24] |
LDCM0402 | CL15 | HEK-293T | C647(0.92); C455(0.76); C188(0.99); C356(1.10) | LDD1606 | [24] |
LDCM0403 | CL16 | HEK-293T | C647(0.94); C455(0.80); C188(0.87); C356(1.31) | LDD1607 | [24] |
LDCM0404 | CL17 | HEK-293T | C647(0.87); C455(0.83); C356(0.81) | LDD1608 | [24] |
LDCM0405 | CL18 | HEK-293T | C647(0.91); C455(0.96); C356(1.20) | LDD1609 | [24] |
LDCM0406 | CL19 | HEK-293T | C647(1.00); C455(0.99); C188(0.98); C356(1.16) | LDD1610 | [24] |
LDCM0407 | CL2 | HEK-293T | C647(1.01); C455(0.89); C356(1.17) | LDD1611 | [24] |
LDCM0408 | CL20 | HEK-293T | C455(0.95); C356(1.20) | LDD1612 | [24] |
LDCM0409 | CL21 | HEK-293T | C647(0.89); C455(0.82); C188(1.30); C356(0.87) | LDD1613 | [24] |
LDCM0410 | CL22 | HEK-293T | C647(0.93); C455(1.00); C356(1.01) | LDD1614 | [24] |
LDCM0411 | CL23 | HEK-293T | C647(0.98); C455(0.98); C188(1.19) | LDD1615 | [24] |
LDCM0412 | CL24 | HEK-293T | C647(1.00); C455(0.99); C356(1.23) | LDD1616 | [24] |
LDCM0413 | CL25 | HEK-293T | C647(0.95); C455(0.87); C188(1.05); C356(1.38) | LDD1617 | [24] |
LDCM0414 | CL26 | HEK-293T | C647(1.02); C455(0.88); C356(1.21) | LDD1618 | [24] |
LDCM0415 | CL27 | HEK-293T | C647(0.97); C455(0.88); C188(1.04); C356(0.95) | LDD1619 | [24] |
LDCM0416 | CL28 | HEK-293T | C647(0.92); C455(1.01); C188(0.89); C356(1.06) | LDD1620 | [24] |
LDCM0417 | CL29 | HEK-293T | C647(0.94); C455(1.03); C356(0.92) | LDD1621 | [24] |
LDCM0418 | CL3 | HEK-293T | C647(1.04); C455(0.86); C188(1.03); C356(1.19) | LDD1622 | [24] |
LDCM0419 | CL30 | HEK-293T | C647(0.99); C455(0.97); C356(1.36) | LDD1623 | [24] |
LDCM0420 | CL31 | HEK-293T | C647(1.07); C455(0.95); C188(1.03); C356(1.10) | LDD1624 | [24] |
LDCM0421 | CL32 | HEK-293T | C455(0.90); C356(1.07) | LDD1625 | [24] |
LDCM0422 | CL33 | HEK-293T | C647(1.10); C455(0.81); C188(1.39); C356(0.80) | LDD1626 | [24] |
LDCM0423 | CL34 | HEK-293T | C647(1.00); C455(0.96); C356(0.70) | LDD1627 | [24] |
LDCM0424 | CL35 | HEK-293T | C647(1.03); C455(1.05); C188(1.17) | LDD1628 | [24] |
LDCM0425 | CL36 | HEK-293T | C647(1.07); C455(0.99); C356(0.95) | LDD1629 | [24] |
LDCM0426 | CL37 | HEK-293T | C647(0.94); C455(0.96); C188(1.11); C356(1.16) | LDD1630 | [24] |
LDCM0428 | CL39 | HEK-293T | C647(0.96); C455(0.84); C188(1.00); C356(0.99) | LDD1632 | [24] |
LDCM0429 | CL4 | HEK-293T | C647(0.86); C455(0.82); C188(0.86); C356(1.07) | LDD1633 | [24] |
LDCM0430 | CL40 | HEK-293T | C647(0.96); C455(0.99); C188(0.87); C356(1.15) | LDD1634 | [24] |
LDCM0431 | CL41 | HEK-293T | C647(0.93); C455(0.99); C356(0.99) | LDD1635 | [24] |
LDCM0432 | CL42 | HEK-293T | C647(1.10); C455(0.98); C356(1.20) | LDD1636 | [24] |
LDCM0433 | CL43 | HEK-293T | C647(1.12); C455(0.91); C188(1.11); C356(0.99) | LDD1637 | [24] |
LDCM0434 | CL44 | HEK-293T | C455(0.90); C356(1.11) | LDD1638 | [24] |
LDCM0435 | CL45 | HEK-293T | C647(1.02); C455(0.91); C188(1.29); C356(1.15) | LDD1639 | [24] |
LDCM0436 | CL46 | HEK-293T | C647(1.15); C455(0.98); C356(0.86) | LDD1640 | [24] |
LDCM0437 | CL47 | HEK-293T | C647(1.00); C455(1.06); C188(1.18) | LDD1641 | [24] |
LDCM0438 | CL48 | HEK-293T | C647(1.09); C455(0.98); C356(1.04) | LDD1642 | [24] |
LDCM0439 | CL49 | HEK-293T | C647(0.97); C455(0.94); C188(1.04); C356(1.29) | LDD1643 | [24] |
LDCM0440 | CL5 | HEK-293T | C647(0.88); C455(0.88); C356(0.82) | LDD1644 | [24] |
LDCM0441 | CL50 | HEK-293T | C647(1.02); C455(0.89); C356(1.15) | LDD1645 | [24] |
LDCM0443 | CL52 | HEK-293T | C647(1.09); C455(0.89); C188(0.90); C356(1.14) | LDD1646 | [24] |
LDCM0444 | CL53 | HEK-293T | C647(0.97); C455(0.87); C356(0.76) | LDD1647 | [24] |
LDCM0445 | CL54 | HEK-293T | C647(0.99); C455(0.83); C356(1.08) | LDD1648 | [24] |
LDCM0446 | CL55 | HEK-293T | C647(1.17); C455(0.86); C188(1.08); C356(1.01) | LDD1649 | [24] |
LDCM0447 | CL56 | HEK-293T | C455(0.89); C356(1.11) | LDD1650 | [24] |
LDCM0448 | CL57 | HEK-293T | C647(1.00); C455(0.80); C188(1.39); C356(1.06) | LDD1651 | [24] |
LDCM0449 | CL58 | HEK-293T | C647(1.02); C455(0.95); C356(0.93) | LDD1652 | [24] |
LDCM0450 | CL59 | HEK-293T | C647(1.06); C455(0.99); C188(1.32) | LDD1653 | [24] |
LDCM0451 | CL6 | HEK-293T | C647(0.95); C455(0.89); C356(1.20) | LDD1654 | [24] |
LDCM0452 | CL60 | HEK-293T | C647(1.08); C455(0.81); C356(1.01) | LDD1655 | [24] |
LDCM0453 | CL61 | HEK-293T | C647(0.91); C455(0.96); C188(1.02); C356(1.16) | LDD1656 | [24] |
LDCM0454 | CL62 | HEK-293T | C647(0.98); C455(0.92); C356(1.08) | LDD1657 | [24] |
LDCM0455 | CL63 | HEK-293T | C647(1.01); C455(0.86); C188(0.94); C356(0.99) | LDD1658 | [24] |
LDCM0456 | CL64 | HEK-293T | C647(0.99); C455(0.79); C188(0.90); C356(1.12) | LDD1659 | [24] |
LDCM0457 | CL65 | HEK-293T | C647(0.93); C455(0.98); C356(0.94) | LDD1660 | [24] |
LDCM0458 | CL66 | HEK-293T | C647(1.02); C455(0.90); C356(1.34) | LDD1661 | [24] |
LDCM0459 | CL67 | HEK-293T | C647(1.04); C455(0.90); C188(1.01); C356(1.12) | LDD1662 | [24] |
LDCM0460 | CL68 | HEK-293T | C455(0.92); C356(1.02) | LDD1663 | [24] |
LDCM0461 | CL69 | HEK-293T | C647(1.08); C455(0.84); C188(1.36); C356(1.01) | LDD1664 | [24] |
LDCM0462 | CL7 | HEK-293T | C647(0.98); C455(1.01); C188(1.15); C356(1.15) | LDD1665 | [24] |
LDCM0463 | CL70 | HEK-293T | C647(1.03); C455(0.98); C356(0.86) | LDD1666 | [24] |
LDCM0464 | CL71 | HEK-293T | C647(0.99); C455(1.03); C188(1.13) | LDD1667 | [24] |
LDCM0465 | CL72 | HEK-293T | C647(1.03); C455(1.01); C356(1.06) | LDD1668 | [24] |
LDCM0466 | CL73 | HEK-293T | C647(0.93); C455(0.92); C188(1.22); C356(1.16) | LDD1669 | [24] |
LDCM0467 | CL74 | HEK-293T | C647(1.05); C455(0.87); C356(1.05) | LDD1670 | [24] |
LDCM0469 | CL76 | HEK-293T | C647(0.97); C455(0.90); C188(0.90); C356(1.19) | LDD1672 | [24] |
LDCM0470 | CL77 | HEK-293T | C647(0.97); C455(0.86); C356(0.98) | LDD1673 | [24] |
LDCM0471 | CL78 | HEK-293T | C647(1.04); C455(0.95); C356(1.02) | LDD1674 | [24] |
LDCM0472 | CL79 | HEK-293T | C647(1.18); C455(0.94); C188(1.01); C356(1.04) | LDD1675 | [24] |
LDCM0473 | CL8 | HEK-293T | C455(0.71); C356(1.16) | LDD1676 | [24] |
LDCM0474 | CL80 | HEK-293T | C455(0.88); C356(1.03) | LDD1677 | [24] |
LDCM0475 | CL81 | HEK-293T | C647(0.93); C455(0.93); C188(1.15); C356(0.80) | LDD1678 | [24] |
LDCM0476 | CL82 | HEK-293T | C647(1.12); C455(0.96); C356(0.87) | LDD1679 | [24] |
LDCM0477 | CL83 | HEK-293T | C647(1.01); C455(1.02); C188(1.30) | LDD1680 | [24] |
LDCM0478 | CL84 | HEK-293T | C647(1.11); C455(1.02); C356(0.99) | LDD1681 | [24] |
LDCM0479 | CL85 | HEK-293T | C647(0.78); C455(0.93); C188(0.98); C356(1.09) | LDD1682 | [24] |
LDCM0480 | CL86 | HEK-293T | C647(0.97); C455(0.88); C356(1.07) | LDD1683 | [24] |
LDCM0481 | CL87 | HEK-293T | C647(0.98); C455(0.88); C188(1.02); C356(1.16) | LDD1684 | [24] |
LDCM0482 | CL88 | HEK-293T | C647(1.03); C455(0.88); C188(0.94); C356(1.17) | LDD1685 | [24] |
LDCM0483 | CL89 | HEK-293T | C647(0.99); C455(0.97); C356(0.96) | LDD1686 | [24] |
LDCM0484 | CL9 | HEK-293T | C647(0.91); C455(0.86); C188(1.28); C356(0.96) | LDD1687 | [24] |
LDCM0485 | CL90 | HEK-293T | C647(1.08); C455(0.82); C356(1.01) | LDD1688 | [24] |
LDCM0486 | CL91 | HEK-293T | C647(1.14); C455(0.85); C188(1.03); C356(1.22) | LDD1689 | [24] |
LDCM0487 | CL92 | HEK-293T | C455(0.76); C356(1.16) | LDD1690 | [24] |
LDCM0488 | CL93 | HEK-293T | C647(0.99); C455(0.82); C188(1.24); C356(0.92) | LDD1691 | [24] |
LDCM0489 | CL94 | HEK-293T | C647(1.08); C455(0.96); C356(0.99) | LDD1692 | [24] |
LDCM0490 | CL95 | HEK-293T | C647(1.09); C455(0.91); C188(1.23) | LDD1693 | [24] |
LDCM0491 | CL96 | HEK-293T | C647(1.05); C455(0.88); C356(1.07) | LDD1694 | [24] |
LDCM0492 | CL97 | HEK-293T | C647(0.99); C455(0.96); C188(1.03); C356(1.26) | LDD1695 | [24] |
LDCM0493 | CL98 | HEK-293T | C647(1.00); C455(0.86); C356(1.06) | LDD1696 | [24] |
LDCM0494 | CL99 | HEK-293T | C647(0.97); C455(0.88); C188(0.97); C356(0.87) | LDD1697 | [24] |
LDCM0165 | Compound 9 | HL-60 | N.A. | LDD0420 | [23] |
LDCM0634 | CY-0357 | Hep-G2 | C455(0.47) | LDD2228 | [12] |
LDCM0495 | E2913 | HEK-293T | C647(0.98); C455(0.83); C188(1.00); C356(1.09) | LDD1698 | [24] |
LDCM0213 | Electrophilic fragment 2 | MDA-MB-231 | C188(6.85); C502(0.87) | LDD1702 | [5] |
LDCM0625 | F8 | Ramos | C455(1.30) | LDD2187 | [25] |
LDCM0572 | Fragment10 | Ramos | C455(0.91) | LDD2189 | [25] |
LDCM0573 | Fragment11 | Ramos | C455(0.85) | LDD2190 | [25] |
LDCM0574 | Fragment12 | Ramos | C455(0.91) | LDD2191 | [25] |
LDCM0575 | Fragment13 | Ramos | C455(0.95) | LDD2192 | [25] |
LDCM0576 | Fragment14 | Ramos | C455(0.83) | LDD2193 | [25] |
LDCM0579 | Fragment20 | Ramos | C455(0.59) | LDD2194 | [25] |
LDCM0580 | Fragment21 | Ramos | C455(0.96) | LDD2195 | [25] |
LDCM0582 | Fragment23 | Ramos | C455(0.95) | LDD2196 | [25] |
LDCM0578 | Fragment27 | Ramos | C455(0.88) | LDD2197 | [25] |
LDCM0586 | Fragment28 | Ramos | C455(0.82) | LDD2198 | [25] |
LDCM0588 | Fragment30 | Ramos | C455(1.00) | LDD2199 | [25] |
LDCM0589 | Fragment31 | Ramos | C455(0.81) | LDD2200 | [25] |
LDCM0590 | Fragment32 | Ramos | C455(0.91) | LDD2201 | [25] |
LDCM0468 | Fragment33 | HEK-293T | C647(0.99); C455(0.89); C188(1.09); C356(1.00) | LDD1671 | [24] |
LDCM0596 | Fragment38 | Ramos | C455(1.04) | LDD2203 | [25] |
LDCM0566 | Fragment4 | Ramos | C455(1.18) | LDD2184 | [25] |
LDCM0427 | Fragment51 | HEK-293T | C647(1.08); C455(0.94); C356(1.22) | LDD1631 | [24] |
LDCM0610 | Fragment52 | Ramos | C455(1.36) | LDD2204 | [25] |
LDCM0614 | Fragment56 | Ramos | C455(1.32) | LDD2205 | [25] |
LDCM0569 | Fragment7 | Ramos | C455(1.33) | LDD2186 | [25] |
LDCM0571 | Fragment9 | Ramos | C455(0.91) | LDD2188 | [25] |
LDCM0107 | IAA | HeLa | N.A. | LDD0221 | [18] |
LDCM0022 | KB02 | HEK-293T | C647(0.90); C455(0.99); C63(0.79); C188(0.86) | LDD1492 | [24] |
LDCM0023 | KB03 | HEK-293T | C647(0.98); C455(1.00); C63(0.98); C188(0.89) | LDD1497 | [24] |
LDCM0024 | KB05 | HMCB | C359(3.35) | LDD3312 | [4] |
LDCM0030 | Luteolin | HEK-293T | 5.05 | LDD0182 | [6] |
LDCM0509 | N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide | MDA-MB-231 | C188(0.70) | LDD2102 | [5] |
LDCM0109 | NEM | HeLa | H211(0.00); C647(0.00) | LDD0223 | [18] |
LDCM0496 | Nucleophilic fragment 11a | MDA-MB-231 | C188(0.50) | LDD2089 | [5] |
LDCM0508 | Nucleophilic fragment 17a | MDA-MB-231 | C188(0.21) | LDD2101 | [5] |
LDCM0513 | Nucleophilic fragment 19b | MDA-MB-231 | C455(0.85) | LDD2106 | [5] |
LDCM0514 | Nucleophilic fragment 20a | MDA-MB-231 | C188(0.96) | LDD2107 | [5] |
LDCM0516 | Nucleophilic fragment 21a | MDA-MB-231 | C188(0.79) | LDD2109 | [5] |
LDCM0518 | Nucleophilic fragment 22a | MDA-MB-231 | C188(0.69) | LDD2111 | [5] |
LDCM0522 | Nucleophilic fragment 24a | MDA-MB-231 | C188(0.29) | LDD2115 | [5] |
LDCM0525 | Nucleophilic fragment 25b | MDA-MB-231 | C455(0.98) | LDD2118 | [5] |
LDCM0526 | Nucleophilic fragment 26a | MDA-MB-231 | C188(1.07) | LDD2119 | [5] |
LDCM0529 | Nucleophilic fragment 27b | MDA-MB-231 | C455(1.01) | LDD2122 | [5] |
LDCM0530 | Nucleophilic fragment 28a | MDA-MB-231 | C188(0.95) | LDD2123 | [5] |
LDCM0532 | Nucleophilic fragment 29a | MDA-MB-231 | C188(1.07); C455(1.25) | LDD2125 | [5] |
LDCM0533 | Nucleophilic fragment 29b | MDA-MB-231 | C455(0.97) | LDD2126 | [5] |
LDCM0534 | Nucleophilic fragment 30a | MDA-MB-231 | C188(1.06); C455(1.28) | LDD2127 | [5] |
LDCM0536 | Nucleophilic fragment 31 | MDA-MB-231 | C188(0.80) | LDD2129 | [5] |
LDCM0541 | Nucleophilic fragment 36 | MDA-MB-231 | C188(0.25) | LDD2134 | [5] |
LDCM0542 | Nucleophilic fragment 37 | MDA-MB-231 | C188(0.83) | LDD2135 | [5] |
LDCM0543 | Nucleophilic fragment 38 | MDA-MB-231 | C502(1.06) | LDD2136 | [5] |
LDCM0544 | Nucleophilic fragment 39 | MDA-MB-231 | C188(1.12) | LDD2137 | [5] |
LDCM0546 | Nucleophilic fragment 40 | MDA-MB-231 | C188(0.52) | LDD2140 | [5] |
LDCM0549 | Nucleophilic fragment 43 | MDA-MB-231 | C188(1.33) | LDD2143 | [5] |
LDCM0550 | Nucleophilic fragment 5a | MDA-MB-231 | C188(1.03) | LDD2144 | [5] |
LDCM0552 | Nucleophilic fragment 6a | MDA-MB-231 | C188(0.65) | LDD2146 | [5] |
LDCM0554 | Nucleophilic fragment 7a | MDA-MB-231 | C188(0.30); C647(0.73) | LDD2148 | [5] |
LDCM0556 | Nucleophilic fragment 8a | MDA-MB-231 | C188(0.44); C455(0.58) | LDD2150 | [5] |
LDCM0032 | Oleacein | HEK-293T | 4.75 | LDD0184 | [6] |
LDCM0131 | RA190 | MM1.R | C356(1.41); C455(1.22) | LDD0304 | [26] |
The Interaction Atlas With This Target
The Protein(s) Related To This Target
Enzyme
Transporter and channel
Other
The Drug(s) Related To This Target
Preclinical
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Sphinx31 | Small molecular drug | D86ILE |
Investigative
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Pmid15925511c13 | Small molecular drug | D0J1JB |
Patented
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Sphinx | Small molecular drug | D0LA9D | |||
Sphinx Scaffold, 3 | Small molecular drug | D0NY4A | |||
Zinc959121 | Small molecular drug | D03OBN |
References