Details of the Target
General Information of Target
Target ID | LDTP04379 | |||||
---|---|---|---|---|---|---|
Target Name | Cyclin-dependent kinase 7 (CDK7) | |||||
Gene Name | CDK7 | |||||
Gene ID | 1022 | |||||
Synonyms |
CAK; CAK1; CDKN7; MO15; STK1; Cyclin-dependent kinase 7; EC 2.7.11.22; EC 2.7.11.23; 39 kDa protein kinase; p39 Mo15; CDK-activating kinase 1; Cell division protein kinase 7; Serine/threonine-protein kinase 1; TFIIH basal transcription factor complex kinase subunit
|
|||||
3D Structure | ||||||
Sequence |
MALDVKSRAKRYEKLDFLGEGQFATVYKARDKNTNQIVAIKKIKLGHRSEAKDGINRTAL
REIKLLQELSHPNIIGLLDAFGHKSNISLVFDFMETDLEVIIKDNSLVLTPSHIKAYMLM TLQGLEYLHQHWILHRDLKPNNLLLDENGVLKLADFGLAKSFGSPNRAYTHQVVTRWYRA PELLFGARMYGVGVDMWAVGCILAELLLRVPFLPGDSDLDQLTRIFETLGTPTEEQWPDM CSLPDYVTFKSFPGIPLHHIFSAAGDDLLDLIQGLFLFNPCARITATQALKMKYFSNRPG PTPGCQLPRPNCPVETLKEQSNPALAIKRKRTEALEQGGLPKKLIF |
|||||
Target Type |
Clinical trial
|
|||||
Target Bioclass |
Enzyme
|
|||||
Family |
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, CDC2/CDKX subfamily
|
|||||
Subcellular location |
Nucleus
|
|||||
Function |
Serine/threonine kinase involved in cell cycle control and in RNA polymerase II-mediated RNA transcription. Cyclin-dependent kinases (CDKs) are activated by the binding to a cyclin and mediate the progression through the cell cycle. Each different complex controls a specific transition between 2 subsequent phases in the cell cycle. Required for both activation and complex formation of CDK1/cyclin-B during G2-M transition, and for activation of CDK2/cyclins during G1-S transition (but not complex formation). CDK7 is the catalytic subunit of the CDK-activating kinase (CAK) complex. Phosphorylates SPT5/SUPT5H, SF1/NR5A1, POLR2A, p53/TP53, CDK1, CDK2, CDK4, CDK6 and CDK11B/CDK11. CAK activates the cyclin-associated kinases CDK1, CDK2, CDK4 and CDK6 by threonine phosphorylation, thus regulating cell cycle progression. CAK complexed to the core-TFIIH basal transcription factor activates RNA polymerase II by serine phosphorylation of the repetitive C-terminal domain (CTD) of its large subunit (POLR2A), allowing its escape from the promoter and elongation of the transcripts. Phosphorylation of POLR2A in complex with DNA promotes transcription initiation by triggering dissociation from DNA. Its expression and activity are constant throughout the cell cycle. Upon DNA damage, triggers p53/TP53 activation by phosphorylation, but is inactivated in turn by p53/TP53; this feedback loop may lead to an arrest of the cell cycle and of the transcription, helping in cell recovery, or to apoptosis. Required for DNA-bound peptides-mediated transcription and cellular growth inhibition.
|
|||||
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 | |
---|---|---|---|---|---|
m-APA Probe Info |
![]() |
15.00 | LDD0402 | [1] | |
TH211 Probe Info |
![]() |
Y169(8.77) | LDD0257 | [2] | |
STPyne Probe Info |
![]() |
K328(6.25) | LDD0277 | [3] | |
IPM Probe Info |
![]() |
C305(0.00); C312(0.00) | LDD0241 | [4] | |
THZ1-DTB Probe Info |
![]() |
C312(8.02) | LDD0460 | [5] | |
BTD Probe Info |
![]() |
C312(0.49) | LDD2089 | [6] | |
AHL-Pu-1 Probe Info |
![]() |
C312(3.25) | LDD0170 | [7] | |
DBIA Probe Info |
![]() |
C305(0.94); C312(0.94) | LDD0078 | [8] | |
ATP probe Probe Info |
![]() |
N.A. | LDD0199 | [9] | |
4-Iodoacetamidophenylacetylene Probe Info |
![]() |
C312(0.00); C305(0.00); C241(0.00) | LDD0038 | [10] | |
IA-alkyne Probe Info |
![]() |
N.A. | LDD0036 | [10] | |
Lodoacetamide azide Probe Info |
![]() |
N.A. | LDD0037 | [10] | |
ATP probe Probe Info |
![]() |
N.A. | LDD0035 | [11] | |
W1 Probe Info |
![]() |
N.A. | LDD0236 | [4] | |
AOyne Probe Info |
![]() |
15.00 | LDD0443 | [12] |
PAL-AfBPP Probe
Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
---|---|---|---|---|---|
Probe 12 Probe Info |
![]() |
N.A. | LDD0420 | [13] |
Competitor(s) Related to This Target
Competitor ID | Name | Cell line | Binding Site(Ratio) | Interaction ID | Ref |
---|---|---|---|---|---|
LDCM0548 | 1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one | MDA-MB-231 | C312(0.97) | LDD2142 | [6] |
LDCM0537 | 2-Cyano-N,N-dimethylacetamide | MDA-MB-231 | C312(0.86) | LDD2130 | [6] |
LDCM0524 | 2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide | MDA-MB-231 | C305(1.01) | LDD2117 | [6] |
LDCM0538 | 4-(Cyanoacetyl)morpholine | MDA-MB-231 | C312(0.54) | LDD2131 | [6] |
LDCM0025 | 4SU-RNA | DM93 | C312(3.25) | LDD0170 | [7] |
LDCM0214 | AC1 | HCT 116 | C305(0.57); C312(0.74) | LDD0531 | [8] |
LDCM0215 | AC10 | HCT 116 | C305(0.86); C312(0.72) | LDD0532 | [8] |
LDCM0216 | AC100 | HCT 116 | C305(1.34); C312(0.87) | LDD0533 | [8] |
LDCM0217 | AC101 | HCT 116 | C305(1.12); C312(0.96) | LDD0534 | [8] |
LDCM0218 | AC102 | HCT 116 | C305(1.01); C312(0.90) | LDD0535 | [8] |
LDCM0219 | AC103 | HCT 116 | C305(1.24); C312(1.20) | LDD0536 | [8] |
LDCM0220 | AC104 | HCT 116 | C305(0.95); C312(0.97) | LDD0537 | [8] |
LDCM0221 | AC105 | HCT 116 | C305(1.03); C312(1.23) | LDD0538 | [8] |
LDCM0222 | AC106 | HCT 116 | C305(1.61); C312(1.28) | LDD0539 | [8] |
LDCM0223 | AC107 | HCT 116 | C305(1.08); C312(1.44) | LDD0540 | [8] |
LDCM0224 | AC108 | HCT 116 | C305(1.47); C312(0.99) | LDD0541 | [8] |
LDCM0225 | AC109 | HCT 116 | C305(0.88); C312(0.85) | LDD0542 | [8] |
LDCM0226 | AC11 | HCT 116 | C305(0.97); C312(0.90) | LDD0543 | [8] |
LDCM0227 | AC110 | HCT 116 | C305(1.10); C312(0.84) | LDD0544 | [8] |
LDCM0228 | AC111 | HCT 116 | C305(0.88); C312(0.94) | LDD0545 | [8] |
LDCM0229 | AC112 | HCT 116 | C305(1.00); C312(1.08) | LDD0546 | [8] |
LDCM0230 | AC113 | HCT 116 | C305(0.94); C312(0.89) | LDD0547 | [8] |
LDCM0231 | AC114 | HCT 116 | C305(0.85); C312(0.84) | LDD0548 | [8] |
LDCM0232 | AC115 | HCT 116 | C305(0.88); C312(0.90) | LDD0549 | [8] |
LDCM0233 | AC116 | HCT 116 | C305(0.92); C312(0.90) | LDD0550 | [8] |
LDCM0234 | AC117 | HCT 116 | C305(1.03); C312(0.95) | LDD0551 | [8] |
LDCM0235 | AC118 | HCT 116 | C305(1.02); C312(0.94) | LDD0552 | [8] |
LDCM0236 | AC119 | HCT 116 | C305(0.91); C312(0.90) | LDD0553 | [8] |
LDCM0237 | AC12 | HCT 116 | C305(0.72); C312(0.63) | LDD0554 | [8] |
LDCM0238 | AC120 | HCT 116 | C305(0.96); C312(0.90) | LDD0555 | [8] |
LDCM0239 | AC121 | HCT 116 | C305(1.03); C312(0.96) | LDD0556 | [8] |
LDCM0240 | AC122 | HCT 116 | C305(1.22); C312(1.11) | LDD0557 | [8] |
LDCM0241 | AC123 | HCT 116 | C305(0.85); C312(0.82) | LDD0558 | [8] |
LDCM0242 | AC124 | HCT 116 | C305(1.00); C312(0.94) | LDD0559 | [8] |
LDCM0243 | AC125 | HCT 116 | C305(1.10); C312(1.02) | LDD0560 | [8] |
LDCM0244 | AC126 | HCT 116 | C305(0.98); C312(0.92) | LDD0561 | [8] |
LDCM0245 | AC127 | HCT 116 | C305(0.90); C312(0.80) | LDD0562 | [8] |
LDCM0246 | AC128 | HCT 116 | C305(0.83); C312(0.70) | LDD0563 | [8] |
LDCM0247 | AC129 | HCT 116 | C305(0.96); C312(0.72) | LDD0564 | [8] |
LDCM0249 | AC130 | HCT 116 | C305(1.08); C312(0.68) | LDD0566 | [8] |
LDCM0250 | AC131 | HCT 116 | C305(1.01); C312(0.93) | LDD0567 | [8] |
LDCM0251 | AC132 | HCT 116 | C305(0.83); C312(0.63) | LDD0568 | [8] |
LDCM0252 | AC133 | HCT 116 | C305(0.87); C312(0.63) | LDD0569 | [8] |
LDCM0253 | AC134 | HCT 116 | C305(1.07); C312(1.10) | LDD0570 | [8] |
LDCM0254 | AC135 | HCT 116 | C305(0.88); C312(0.68) | LDD0571 | [8] |
LDCM0255 | AC136 | HCT 116 | C305(0.98); C312(0.72) | LDD0572 | [8] |
LDCM0256 | AC137 | HCT 116 | C305(0.96); C312(0.81) | LDD0573 | [8] |
LDCM0257 | AC138 | HCT 116 | C305(1.23); C312(1.32) | LDD0574 | [8] |
LDCM0258 | AC139 | HCT 116 | C305(0.99); C312(0.78) | LDD0575 | [8] |
LDCM0259 | AC14 | HCT 116 | C305(0.86); C312(0.92) | LDD0576 | [8] |
LDCM0260 | AC140 | HCT 116 | C305(1.07); C312(1.00) | LDD0577 | [8] |
LDCM0261 | AC141 | HCT 116 | C305(1.18); C312(1.02) | LDD0578 | [8] |
LDCM0262 | AC142 | HCT 116 | C305(1.09); C312(0.78) | LDD0579 | [8] |
LDCM0263 | AC143 | HCT 116 | C305(0.98); C312(1.00) | LDD0580 | [8] |
LDCM0264 | AC144 | HCT 116 | C305(0.97); C312(1.17) | LDD0581 | [8] |
LDCM0265 | AC145 | HCT 116 | C305(0.87); C312(1.09) | LDD0582 | [8] |
LDCM0266 | AC146 | HCT 116 | C312(0.94); C305(0.95) | LDD0583 | [8] |
LDCM0267 | AC147 | HCT 116 | C305(0.88); C312(1.09) | LDD0584 | [8] |
LDCM0268 | AC148 | HCT 116 | C305(0.93); C312(1.21) | LDD0585 | [8] |
LDCM0269 | AC149 | HCT 116 | C305(0.98); C312(1.07) | LDD0586 | [8] |
LDCM0270 | AC15 | HCT 116 | C312(0.65); C305(0.76) | LDD0587 | [8] |
LDCM0271 | AC150 | HCT 116 | C305(0.97); C312(1.05) | LDD0588 | [8] |
LDCM0272 | AC151 | HCT 116 | C312(0.84); C305(0.88) | LDD0589 | [8] |
LDCM0273 | AC152 | HCT 116 | C305(0.88); C312(1.02) | LDD0590 | [8] |
LDCM0274 | AC153 | HCT 116 | C305(1.01); C312(1.22) | LDD0591 | [8] |
LDCM0621 | AC154 | HCT 116 | C305(0.81); C312(0.91) | LDD2158 | [8] |
LDCM0622 | AC155 | HCT 116 | C305(0.94); C312(1.10) | LDD2159 | [8] |
LDCM0623 | AC156 | HCT 116 | C305(0.84); C312(0.92) | LDD2160 | [8] |
LDCM0624 | AC157 | HCT 116 | C305(0.92); C312(0.93) | LDD2161 | [8] |
LDCM0276 | AC17 | HCT 116 | C305(1.08); C312(1.15) | LDD0593 | [8] |
LDCM0277 | AC18 | HCT 116 | C305(0.89); C312(1.04) | LDD0594 | [8] |
LDCM0278 | AC19 | HCT 116 | C305(1.09); C312(1.17) | LDD0595 | [8] |
LDCM0279 | AC2 | HCT 116 | C305(0.67); C312(0.85) | LDD0596 | [8] |
LDCM0280 | AC20 | HCT 116 | C305(1.13); C312(1.18) | LDD0597 | [8] |
LDCM0281 | AC21 | HCT 116 | C305(0.74); C312(1.05) | LDD0598 | [8] |
LDCM0282 | AC22 | HCT 116 | C305(1.02); C312(1.24) | LDD0599 | [8] |
LDCM0283 | AC23 | HCT 116 | C305(0.97); C312(1.09) | LDD0600 | [8] |
LDCM0284 | AC24 | HCT 116 | C312(1.05); C305(1.07) | LDD0601 | [8] |
LDCM0285 | AC25 | HCT 116 | C312(0.60); C305(0.62) | LDD0602 | [8] |
LDCM0286 | AC26 | HCT 116 | C312(0.71); C305(0.82) | LDD0603 | [8] |
LDCM0287 | AC27 | HCT 116 | C312(0.78); C305(0.85) | LDD0604 | [8] |
LDCM0288 | AC28 | HCT 116 | C312(0.79); C305(0.92) | LDD0605 | [8] |
LDCM0289 | AC29 | HCT 116 | C305(0.73); C312(0.77) | LDD0606 | [8] |
LDCM0290 | AC3 | HCT 116 | C305(0.55); C312(0.80) | LDD0607 | [8] |
LDCM0291 | AC30 | HCT 116 | C305(0.94); C312(1.03) | LDD0608 | [8] |
LDCM0292 | AC31 | HCT 116 | C312(0.64); C305(0.71) | LDD0609 | [8] |
LDCM0293 | AC32 | HCT 116 | C312(0.77); C305(0.85) | LDD0610 | [8] |
LDCM0294 | AC33 | HCT 116 | C305(0.70); C312(0.74) | LDD0611 | [8] |
LDCM0295 | AC34 | HCT 116 | C305(0.79); C312(0.89) | LDD0612 | [8] |
LDCM0296 | AC35 | HCT 116 | C312(0.71); C305(0.89) | LDD0613 | [8] |
LDCM0297 | AC36 | HCT 116 | C312(0.85); C305(0.98) | LDD0614 | [8] |
LDCM0298 | AC37 | HCT 116 | C312(0.88); C305(1.02) | LDD0615 | [8] |
LDCM0299 | AC38 | HCT 116 | C312(0.86); C305(0.99) | LDD0616 | [8] |
LDCM0300 | AC39 | HCT 116 | C312(0.69); C305(0.95) | LDD0617 | [8] |
LDCM0301 | AC4 | HCT 116 | C305(0.55); C312(0.82) | LDD0618 | [8] |
LDCM0302 | AC40 | HCT 116 | C305(1.03); C312(1.11) | LDD0619 | [8] |
LDCM0303 | AC41 | HCT 116 | C305(1.20); C312(1.90) | LDD0620 | [8] |
LDCM0304 | AC42 | HCT 116 | C305(1.15); C312(1.82) | LDD0621 | [8] |
LDCM0305 | AC43 | HCT 116 | C305(1.39); C312(1.85) | LDD0622 | [8] |
LDCM0306 | AC44 | HCT 116 | C305(1.13); C312(1.75) | LDD0623 | [8] |
LDCM0307 | AC45 | HCT 116 | C305(1.19); C312(1.61) | LDD0624 | [8] |
LDCM0308 | AC46 | HCT 116 | C312(0.96); C305(1.03) | LDD0625 | [8] |
LDCM0309 | AC47 | HCT 116 | C305(1.10); C312(1.16) | LDD0626 | [8] |
LDCM0310 | AC48 | HCT 116 | C305(0.94); C312(0.94) | LDD0627 | [8] |
LDCM0311 | AC49 | HCT 116 | C312(0.97); C305(1.04) | LDD0628 | [8] |
LDCM0312 | AC5 | HCT 116 | C305(0.56); C312(0.70) | LDD0629 | [8] |
LDCM0313 | AC50 | HCT 116 | C305(1.02); C312(1.17) | LDD0630 | [8] |
LDCM0314 | AC51 | HCT 116 | C305(1.22); C312(1.47) | LDD0631 | [8] |
LDCM0315 | AC52 | HCT 116 | C312(1.01); C305(1.03) | LDD0632 | [8] |
LDCM0316 | AC53 | HCT 116 | C305(1.58); C312(2.09) | LDD0633 | [8] |
LDCM0317 | AC54 | HCT 116 | C305(1.10); C312(1.16) | LDD0634 | [8] |
LDCM0318 | AC55 | HCT 116 | C305(1.28); C312(1.50) | LDD0635 | [8] |
LDCM0319 | AC56 | HCT 116 | C305(1.46); C312(2.00) | LDD0636 | [8] |
LDCM0320 | AC57 | HCT 116 | C305(0.91); C312(0.96) | LDD0637 | [8] |
LDCM0321 | AC58 | HCT 116 | C305(1.00); C312(1.07) | LDD0638 | [8] |
LDCM0322 | AC59 | HCT 116 | C305(1.01); C312(1.21) | LDD0639 | [8] |
LDCM0323 | AC6 | HCT 116 | C312(0.98); C305(1.01) | LDD0640 | [8] |
LDCM0324 | AC60 | HCT 116 | C305(1.02); C312(1.04) | LDD0641 | [8] |
LDCM0325 | AC61 | HCT 116 | C312(1.00); C305(1.02) | LDD0642 | [8] |
LDCM0326 | AC62 | HCT 116 | C305(1.10); C312(1.45) | LDD0643 | [8] |
LDCM0327 | AC63 | HCT 116 | C305(0.98); C312(1.03) | LDD0644 | [8] |
LDCM0328 | AC64 | HCT 116 | C305(0.79); C312(0.90) | LDD0645 | [8] |
LDCM0329 | AC65 | HCT 116 | C312(0.82); C305(1.15) | LDD0646 | [8] |
LDCM0330 | AC66 | HCT 116 | C312(0.82); C305(1.15) | LDD0647 | [8] |
LDCM0331 | AC67 | HCT 116 | C305(0.93); C312(1.00) | LDD0648 | [8] |
LDCM0332 | AC68 | HCT 116 | C305(1.02); C312(1.44) | LDD0649 | [8] |
LDCM0333 | AC69 | HCT 116 | C305(0.75); C312(1.13) | LDD0650 | [8] |
LDCM0334 | AC7 | HCT 116 | C305(0.99); C312(1.12) | LDD0651 | [8] |
LDCM0335 | AC70 | HCT 116 | C305(1.09); C312(1.27) | LDD0652 | [8] |
LDCM0336 | AC71 | HCT 116 | C305(1.03); C312(1.26) | LDD0653 | [8] |
LDCM0337 | AC72 | HCT 116 | C305(0.98); C312(1.33) | LDD0654 | [8] |
LDCM0338 | AC73 | HCT 116 | C305(1.22); C312(1.35) | LDD0655 | [8] |
LDCM0339 | AC74 | HCT 116 | C305(0.93); C312(1.14) | LDD0656 | [8] |
LDCM0340 | AC75 | HCT 116 | C305(1.14); C312(1.24) | LDD0657 | [8] |
LDCM0341 | AC76 | HCT 116 | C305(0.91); C312(1.12) | LDD0658 | [8] |
LDCM0342 | AC77 | HCT 116 | C305(0.99); C312(1.46) | LDD0659 | [8] |
LDCM0343 | AC78 | HCT 116 | C305(0.90); C312(1.14) | LDD0660 | [8] |
LDCM0344 | AC79 | HCT 116 | C305(1.11); C312(1.56) | LDD0661 | [8] |
LDCM0345 | AC8 | HCT 116 | C312(0.87); C305(0.96) | LDD0662 | [8] |
LDCM0346 | AC80 | HCT 116 | C312(0.95); C305(1.06) | LDD0663 | [8] |
LDCM0347 | AC81 | HCT 116 | C305(1.02); C312(1.28) | LDD0664 | [8] |
LDCM0348 | AC82 | HCT 116 | C305(1.14); C312(1.40) | LDD0665 | [8] |
LDCM0349 | AC83 | HCT 116 | C312(0.80); C305(1.10) | LDD0666 | [8] |
LDCM0350 | AC84 | HCT 116 | C305(0.94); C312(0.99) | LDD0667 | [8] |
LDCM0351 | AC85 | HCT 116 | C312(0.97); C305(1.14) | LDD0668 | [8] |
LDCM0352 | AC86 | HCT 116 | C312(0.96); C305(1.34) | LDD0669 | [8] |
LDCM0353 | AC87 | HCT 116 | C312(0.90); C305(0.90) | LDD0670 | [8] |
LDCM0354 | AC88 | HCT 116 | C312(0.95); C305(1.06) | LDD0671 | [8] |
LDCM0355 | AC89 | HCT 116 | C312(0.89); C305(0.97) | LDD0672 | [8] |
LDCM0357 | AC90 | HCT 116 | C312(1.11); C305(1.20) | LDD0674 | [8] |
LDCM0358 | AC91 | HCT 116 | C312(0.96); C305(1.04) | LDD0675 | [8] |
LDCM0359 | AC92 | HCT 116 | C312(1.12); C305(1.20) | LDD0676 | [8] |
LDCM0360 | AC93 | HCT 116 | C312(0.88); C305(1.11) | LDD0677 | [8] |
LDCM0361 | AC94 | HCT 116 | C312(1.06); C305(1.30) | LDD0678 | [8] |
LDCM0362 | AC95 | HCT 116 | C312(1.02); C305(1.34) | LDD0679 | [8] |
LDCM0363 | AC96 | HCT 116 | C305(1.00); C312(1.12) | LDD0680 | [8] |
LDCM0364 | AC97 | HCT 116 | C312(1.15); C305(1.20) | LDD0681 | [8] |
LDCM0365 | AC98 | HCT 116 | C305(1.36); C312(1.36) | LDD0682 | [8] |
LDCM0366 | AC99 | HCT 116 | C312(0.93); C305(1.36) | LDD0683 | [8] |
LDCM0248 | AKOS034007472 | HCT 116 | C305(0.69); C312(0.65) | LDD0565 | [8] |
LDCM0356 | AKOS034007680 | HCT 116 | C305(0.83); C312(0.86) | LDD0673 | [8] |
LDCM0275 | AKOS034007705 | HCT 116 | C312(0.74); C305(0.84) | LDD0592 | [8] |
LDCM0156 | Aniline | NCI-H1299 | 13.36 | LDD0403 | [1] |
LDCM0020 | ARS-1620 | HCC44 | C305(0.94); C312(0.94) | LDD0078 | [8] |
LDCM0498 | BS-3668 | MDA-MB-231 | C312(0.42) | LDD2091 | [6] |
LDCM0367 | CL1 | HCT 116 | C312(0.98); C305(1.10) | LDD0684 | [8] |
LDCM0368 | CL10 | HCT 116 | C305(0.93); C312(0.95) | LDD0685 | [8] |
LDCM0369 | CL100 | HCT 116 | C305(0.59); C312(0.84) | LDD0686 | [8] |
LDCM0370 | CL101 | HCT 116 | C305(1.00); C312(1.14) | LDD0687 | [8] |
LDCM0371 | CL102 | HCT 116 | C305(0.83); C312(0.98) | LDD0688 | [8] |
LDCM0372 | CL103 | HCT 116 | C312(0.92); C305(1.07) | LDD0689 | [8] |
LDCM0373 | CL104 | HCT 116 | C305(0.73); C312(0.82) | LDD0690 | [8] |
LDCM0374 | CL105 | HCT 116 | C305(1.02); C312(1.12) | LDD0691 | [8] |
LDCM0375 | CL106 | HCT 116 | C305(0.88); C312(1.11) | LDD0692 | [8] |
LDCM0376 | CL107 | HCT 116 | C312(1.09); C305(1.39) | LDD0693 | [8] |
LDCM0377 | CL108 | HCT 116 | C305(1.08); C312(1.29) | LDD0694 | [8] |
LDCM0378 | CL109 | HCT 116 | C305(1.21); C312(1.26) | LDD0695 | [8] |
LDCM0379 | CL11 | HCT 116 | C312(0.91); C305(0.92) | LDD0696 | [8] |
LDCM0380 | CL110 | HCT 116 | C305(1.03); C312(1.17) | LDD0697 | [8] |
LDCM0381 | CL111 | HCT 116 | C305(1.02); C312(1.17) | LDD0698 | [8] |
LDCM0382 | CL112 | HCT 116 | C312(0.74); C305(0.76) | LDD0699 | [8] |
LDCM0383 | CL113 | HCT 116 | C305(0.79); C312(0.84) | LDD0700 | [8] |
LDCM0384 | CL114 | HCT 116 | C312(0.77); C305(0.80) | LDD0701 | [8] |
LDCM0385 | CL115 | HCT 116 | C312(0.73); C305(0.75) | LDD0702 | [8] |
LDCM0386 | CL116 | HCT 116 | C312(0.65); C305(0.67) | LDD0703 | [8] |
LDCM0387 | CL117 | HCT 116 | C305(1.25); C312(2.28) | LDD0704 | [8] |
LDCM0388 | CL118 | HCT 116 | C312(0.82); C305(1.18) | LDD0705 | [8] |
LDCM0389 | CL119 | HCT 116 | C312(0.87); C305(1.07) | LDD0706 | [8] |
LDCM0390 | CL12 | HCT 116 | C312(1.06); C305(1.09) | LDD0707 | [8] |
LDCM0391 | CL120 | HCT 116 | C312(1.12); C305(1.19) | LDD0708 | [8] |
LDCM0392 | CL121 | HCT 116 | C305(1.17); C312(1.23) | LDD0709 | [8] |
LDCM0393 | CL122 | HCT 116 | C305(1.12); C312(1.23) | LDD0710 | [8] |
LDCM0394 | CL123 | HCT 116 | C305(0.96); C312(1.26) | LDD0711 | [8] |
LDCM0395 | CL124 | HCT 116 | C312(1.04); C305(1.08) | LDD0712 | [8] |
LDCM0396 | CL125 | HCT 116 | C312(0.96); C305(1.52) | LDD0713 | [8] |
LDCM0397 | CL126 | HCT 116 | C312(1.19); C305(1.46) | LDD0714 | [8] |
LDCM0398 | CL127 | HCT 116 | C312(1.11); C305(1.59) | LDD0715 | [8] |
LDCM0399 | CL128 | HCT 116 | C312(1.01); C305(1.07) | LDD0716 | [8] |
LDCM0400 | CL13 | HCT 116 | C312(0.86); C305(0.87) | LDD0717 | [8] |
LDCM0401 | CL14 | HCT 116 | C305(0.89); C312(0.94) | LDD0718 | [8] |
LDCM0402 | CL15 | HCT 116 | C305(0.93); C312(0.94) | LDD0719 | [8] |
LDCM0403 | CL16 | HCT 116 | C312(1.06); C305(1.53) | LDD0720 | [8] |
LDCM0404 | CL17 | HCT 116 | C312(1.25); C305(1.39) | LDD0721 | [8] |
LDCM0405 | CL18 | HCT 116 | C312(1.09); C305(1.26) | LDD0722 | [8] |
LDCM0406 | CL19 | HCT 116 | C312(1.08); C305(1.17) | LDD0723 | [8] |
LDCM0407 | CL2 | HCT 116 | C305(1.04); C312(1.16) | LDD0724 | [8] |
LDCM0408 | CL20 | HCT 116 | C305(1.14); C312(1.21) | LDD0725 | [8] |
LDCM0409 | CL21 | HCT 116 | C312(1.10); C305(1.20) | LDD0726 | [8] |
LDCM0410 | CL22 | HCT 116 | C305(1.41); C312(1.44) | LDD0727 | [8] |
LDCM0411 | CL23 | HCT 116 | C312(1.16); C305(1.46) | LDD0728 | [8] |
LDCM0412 | CL24 | HCT 116 | C312(1.03); C305(1.48) | LDD0729 | [8] |
LDCM0413 | CL25 | HCT 116 | C305(1.47); C312(1.09) | LDD0730 | [8] |
LDCM0414 | CL26 | HCT 116 | C305(1.52); C312(1.07) | LDD0731 | [8] |
LDCM0415 | CL27 | HCT 116 | C305(1.76); C312(1.04) | LDD0732 | [8] |
LDCM0416 | CL28 | HCT 116 | C305(1.54); C312(1.03) | LDD0733 | [8] |
LDCM0417 | CL29 | HCT 116 | C305(1.65); C312(1.26) | LDD0734 | [8] |
LDCM0418 | CL3 | HCT 116 | C305(0.87); C312(0.89) | LDD0735 | [8] |
LDCM0419 | CL30 | HCT 116 | C305(1.33); C312(1.06) | LDD0736 | [8] |
LDCM0420 | CL31 | HCT 116 | C305(1.01); C312(0.93) | LDD0737 | [8] |
LDCM0421 | CL32 | HCT 116 | C305(1.67); C312(1.28) | LDD0738 | [8] |
LDCM0422 | CL33 | HCT 116 | C305(1.15); C312(1.24) | LDD0739 | [8] |
LDCM0423 | CL34 | HCT 116 | C305(1.28); C312(1.15) | LDD0740 | [8] |
LDCM0424 | CL35 | HCT 116 | C305(1.36); C312(1.08) | LDD0741 | [8] |
LDCM0425 | CL36 | HCT 116 | C305(1.14); C312(0.90) | LDD0742 | [8] |
LDCM0426 | CL37 | HCT 116 | C305(1.08); C312(0.99) | LDD0743 | [8] |
LDCM0428 | CL39 | HCT 116 | C305(1.18); C312(1.08) | LDD0745 | [8] |
LDCM0429 | CL4 | HCT 116 | C305(1.06); C312(0.97) | LDD0746 | [8] |
LDCM0430 | CL40 | HCT 116 | C305(1.02); C312(0.97) | LDD0747 | [8] |
LDCM0431 | CL41 | HCT 116 | C305(0.99); C312(0.81) | LDD0748 | [8] |
LDCM0432 | CL42 | HCT 116 | C305(0.87); C312(0.81) | LDD0749 | [8] |
LDCM0433 | CL43 | HCT 116 | C305(1.18); C312(1.15) | LDD0750 | [8] |
LDCM0434 | CL44 | HCT 116 | C305(1.27); C312(1.11) | LDD0751 | [8] |
LDCM0435 | CL45 | HCT 116 | C305(1.32); C312(1.05) | LDD0752 | [8] |
LDCM0436 | CL46 | HCT 116 | C305(1.22); C312(1.29) | LDD0753 | [8] |
LDCM0437 | CL47 | HCT 116 | C305(1.64); C312(1.58) | LDD0754 | [8] |
LDCM0438 | CL48 | HCT 116 | C305(1.11); C312(1.19) | LDD0755 | [8] |
LDCM0439 | CL49 | HCT 116 | C305(1.51); C312(1.48) | LDD0756 | [8] |
LDCM0440 | CL5 | HCT 116 | C305(0.97); C312(0.96) | LDD0757 | [8] |
LDCM0441 | CL50 | HCT 116 | C305(0.99); C312(0.90) | LDD0758 | [8] |
LDCM0442 | CL51 | HCT 116 | C305(1.21); C312(1.17) | LDD0759 | [8] |
LDCM0443 | CL52 | HCT 116 | C305(1.30); C312(1.40) | LDD0760 | [8] |
LDCM0444 | CL53 | HCT 116 | C305(1.07); C312(1.09) | LDD0761 | [8] |
LDCM0445 | CL54 | HCT 116 | C305(0.96); C312(1.04) | LDD0762 | [8] |
LDCM0446 | CL55 | HCT 116 | C305(0.93); C312(0.85) | LDD0763 | [8] |
LDCM0447 | CL56 | HCT 116 | C305(0.89); C312(0.92) | LDD0764 | [8] |
LDCM0448 | CL57 | HCT 116 | C305(1.11); C312(1.14) | LDD0765 | [8] |
LDCM0449 | CL58 | HCT 116 | C305(1.43); C312(1.33) | LDD0766 | [8] |
LDCM0450 | CL59 | HCT 116 | C305(1.12); C312(1.08) | LDD0767 | [8] |
LDCM0451 | CL6 | HCT 116 | C305(1.24); C312(1.08) | LDD0768 | [8] |
LDCM0452 | CL60 | HCT 116 | C305(1.35); C312(1.32) | LDD0769 | [8] |
LDCM0453 | CL61 | HCT 116 | C305(1.36); C312(0.81) | LDD0770 | [8] |
LDCM0454 | CL62 | HCT 116 | C305(1.05); C312(0.88) | LDD0771 | [8] |
LDCM0455 | CL63 | HCT 116 | C305(0.70); C312(0.79) | LDD0772 | [8] |
LDCM0456 | CL64 | HCT 116 | C305(0.90); C312(0.80) | LDD0773 | [8] |
LDCM0457 | CL65 | HCT 116 | C305(0.89); C312(0.74) | LDD0774 | [8] |
LDCM0458 | CL66 | HCT 116 | C305(0.76); C312(0.78) | LDD0775 | [8] |
LDCM0459 | CL67 | HCT 116 | C305(0.61); C312(0.74) | LDD0776 | [8] |
LDCM0460 | CL68 | HCT 116 | C305(0.76); C312(1.02) | LDD0777 | [8] |
LDCM0461 | CL69 | HCT 116 | C305(0.81); C312(0.85) | LDD0778 | [8] |
LDCM0462 | CL7 | HCT 116 | C305(1.08); C312(0.99) | LDD0779 | [8] |
LDCM0463 | CL70 | HCT 116 | C305(0.85); C312(0.80) | LDD0780 | [8] |
LDCM0464 | CL71 | HCT 116 | C305(0.84); C312(0.86) | LDD0781 | [8] |
LDCM0465 | CL72 | HCT 116 | C305(0.86); C312(0.94) | LDD0782 | [8] |
LDCM0466 | CL73 | HCT 116 | C305(0.80); C312(0.79) | LDD0783 | [8] |
LDCM0467 | CL74 | HCT 116 | C305(0.82); C312(0.83) | LDD0784 | [8] |
LDCM0469 | CL76 | HCT 116 | C305(0.70); C312(0.81) | LDD0786 | [8] |
LDCM0470 | CL77 | HCT 116 | C305(0.83); C312(0.94) | LDD0787 | [8] |
LDCM0471 | CL78 | HCT 116 | C305(0.93); C312(0.99) | LDD0788 | [8] |
LDCM0472 | CL79 | HCT 116 | C305(0.77); C312(0.78) | LDD0789 | [8] |
LDCM0473 | CL8 | HCT 116 | C305(1.01); C312(0.99) | LDD0790 | [8] |
LDCM0474 | CL80 | HCT 116 | C305(0.82); C312(0.79) | LDD0791 | [8] |
LDCM0475 | CL81 | HCT 116 | C305(0.88); C312(0.84) | LDD0792 | [8] |
LDCM0476 | CL82 | HCT 116 | C305(0.78); C312(0.80) | LDD0793 | [8] |
LDCM0477 | CL83 | HCT 116 | C305(0.72); C312(0.80) | LDD0794 | [8] |
LDCM0478 | CL84 | HCT 116 | C305(0.76); C312(0.79) | LDD0795 | [8] |
LDCM0479 | CL85 | HCT 116 | C305(0.68); C312(0.77) | LDD0796 | [8] |
LDCM0480 | CL86 | HCT 116 | C305(0.70); C312(0.68) | LDD0797 | [8] |
LDCM0481 | CL87 | HCT 116 | C305(0.74); C312(0.67) | LDD0798 | [8] |
LDCM0482 | CL88 | HCT 116 | C305(0.66); C312(0.64) | LDD0799 | [8] |
LDCM0483 | CL89 | HCT 116 | C305(0.74); C312(0.76) | LDD0800 | [8] |
LDCM0484 | CL9 | HCT 116 | C305(1.09); C312(1.12) | LDD0801 | [8] |
LDCM0485 | CL90 | HCT 116 | C305(0.78); C312(0.92) | LDD0802 | [8] |
LDCM0486 | CL91 | HCT 116 | C305(0.89); C312(0.97) | LDD0803 | [8] |
LDCM0487 | CL92 | HCT 116 | C305(0.95); C312(1.00) | LDD0804 | [8] |
LDCM0488 | CL93 | HCT 116 | C305(0.73); C312(0.85) | LDD0805 | [8] |
LDCM0489 | CL94 | HCT 116 | C305(0.73); C312(0.86) | LDD0806 | [8] |
LDCM0490 | CL95 | HCT 116 | C305(0.85); C312(0.87) | LDD0807 | [8] |
LDCM0491 | CL96 | HCT 116 | C305(0.73); C312(0.81) | LDD0808 | [8] |
LDCM0492 | CL97 | HCT 116 | C305(0.70); C312(0.80) | LDD0809 | [8] |
LDCM0493 | CL98 | HCT 116 | C305(0.69); C312(0.77) | LDD0810 | [8] |
LDCM0494 | CL99 | HCT 116 | C305(0.60); C312(0.79) | LDD0811 | [8] |
LDCM0165 | Compound 9 | HL-60 | N.A. | LDD0420 | [13] |
LDCM0495 | E2913 | HEK-293T | C305(0.94); C312(0.70); C241(0.96) | LDD1698 | [14] |
LDCM0213 | Electrophilic fragment 2 | MDA-MB-231 | C312(1.07); C305(1.00) | LDD1702 | [6] |
LDCM0468 | Fragment33 | HCT 116 | C305(0.85); C312(0.86) | LDD0785 | [8] |
LDCM0427 | Fragment51 | HCT 116 | C305(1.04); C312(0.89) | LDD0744 | [8] |
LDCM0022 | KB02 | HCT 116 | C312(1.18) | LDD0080 | [8] |
LDCM0023 | KB03 | HCT 116 | C312(1.23) | LDD0081 | [8] |
LDCM0024 | KB05 | HCT 116 | C312(1.42) | LDD0082 | [8] |
LDCM0509 | N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide | MDA-MB-231 | C312(1.10) | LDD2102 | [6] |
LDCM0528 | N-(4-bromophenyl)-2-cyano-N-phenylacetamide | MDA-MB-231 | C312(0.82) | LDD2121 | [6] |
LDCM0496 | Nucleophilic fragment 11a | MDA-MB-231 | C312(0.49) | LDD2089 | [6] |
LDCM0499 | Nucleophilic fragment 12b | MDA-MB-231 | C312(0.76) | LDD2092 | [6] |
LDCM0500 | Nucleophilic fragment 13a | MDA-MB-231 | C305(1.05) | LDD2093 | [6] |
LDCM0501 | Nucleophilic fragment 13b | MDA-MB-231 | C312(0.90) | LDD2094 | [6] |
LDCM0505 | Nucleophilic fragment 15b | MDA-MB-231 | C312(0.92) | LDD2098 | [6] |
LDCM0506 | Nucleophilic fragment 16a | MDA-MB-231 | C312(0.91) | LDD2099 | [6] |
LDCM0507 | Nucleophilic fragment 16b | MDA-MB-231 | C312(0.82) | LDD2100 | [6] |
LDCM0512 | Nucleophilic fragment 19a | MDA-MB-231 | C312(1.23) | LDD2105 | [6] |
LDCM0514 | Nucleophilic fragment 20a | MDA-MB-231 | C305(0.92) | LDD2107 | [6] |
LDCM0516 | Nucleophilic fragment 21a | MDA-MB-231 | C312(1.41); C305(1.11) | LDD2109 | [6] |
LDCM0518 | Nucleophilic fragment 22a | MDA-MB-231 | C312(0.78) | LDD2111 | [6] |
LDCM0521 | Nucleophilic fragment 23b | MDA-MB-231 | C312(0.55) | LDD2114 | [6] |
LDCM0525 | Nucleophilic fragment 25b | MDA-MB-231 | C312(1.25) | LDD2118 | [6] |
LDCM0526 | Nucleophilic fragment 26a | MDA-MB-231 | C312(2.16) | LDD2119 | [6] |
LDCM0529 | Nucleophilic fragment 27b | MDA-MB-231 | C312(0.59) | LDD2122 | [6] |
LDCM0530 | Nucleophilic fragment 28a | MDA-MB-231 | C312(0.76); C305(0.80) | LDD2123 | [6] |
LDCM0531 | Nucleophilic fragment 28b | MDA-MB-231 | C312(1.20) | LDD2124 | [6] |
LDCM0532 | Nucleophilic fragment 29a | MDA-MB-231 | C312(0.87); C305(1.02) | LDD2125 | [6] |
LDCM0533 | Nucleophilic fragment 29b | MDA-MB-231 | C312(1.10) | LDD2126 | [6] |
LDCM0534 | Nucleophilic fragment 30a | MDA-MB-231 | C312(0.92) | LDD2127 | [6] |
LDCM0536 | Nucleophilic fragment 31 | MDA-MB-231 | C312(0.82) | LDD2129 | [6] |
LDCM0543 | Nucleophilic fragment 38 | MDA-MB-231 | C312(1.05); C305(0.96) | LDD2136 | [6] |
LDCM0544 | Nucleophilic fragment 39 | MDA-MB-231 | C312(0.95); C305(0.97) | LDD2137 | [6] |
LDCM0546 | Nucleophilic fragment 40 | MDA-MB-231 | C312(0.83) | LDD2140 | [6] |
LDCM0547 | Nucleophilic fragment 41 | MDA-MB-231 | C312(0.79) | LDD2141 | [6] |
LDCM0551 | Nucleophilic fragment 5b | MDA-MB-231 | C312(1.21) | LDD2145 | [6] |
LDCM0555 | Nucleophilic fragment 7b | MDA-MB-231 | C312(1.72) | LDD2149 | [6] |
LDCM0556 | Nucleophilic fragment 8a | MDA-MB-231 | C312(0.64) | LDD2150 | [6] |
LDCM0021 | THZ1 | HCT 116 | C312(20.00) | LDD0079 | [8] |
The Interaction Atlas With This Target
The Protein(s) Related To This Target
Enzyme
Transporter and channel
Protein name | Family | Uniprot ID | |||
---|---|---|---|---|---|
Heat shock protein HSP 90-beta (HSP90AB1) | Heat shock protein 90 family | P08238 |
Other
Protein name | Family | Uniprot ID | |||
---|---|---|---|---|---|
Transcription elongation factor SPT5 (SUPT5H) | SPT5 family | O00267 |
The Drug(s) Related To This Target
Approved
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Trilaciclib | . | DB15442 |
Phase 2
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
R-roscovitine | Small molecular drug | D05ADP |
Phase 1
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
Btx-a51 | Small molecular drug | D5VMP4 | |||
Ly3405105 | Small molecular drug | D0VIG4 | |||
Sns-032 | Small molecular drug | D0S5RC | |||
Sy-5609 | Small molecular drug | DJ9WC4 | |||
Sy-1365 | . | D09OHR |
Investigative
Patented
Discontinued
Drug Name | Drug Type | External ID | |||
---|---|---|---|---|---|
R547 | Small molecular drug | D04FHB | |||
Zk 304709 | Small molecular drug | D00VBT |
References