General Information of Target

Target ID LDTP03546
Target Name Translocator protein (TSPO)
Gene Name TSPO
Gene ID 706
Synonyms
BZRP; MBR; Translocator protein; Mitochondrial benzodiazepine receptor; PKBS; Peripheral-type benzodiazepine receptor; PBR
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAPPWVPAMGFTLAPSLGCFVGSRFVHGEGLRWYAGLQKPSWHPPHWVLGPVWGTLYSAM
GYGSYLVWKELGGFTEKAVVPLGLYTGQLALNWAWPPIFFGARQMGWALVDLLLVSGAAA
ATTVAWYQVSPLAARLLYPYLAWLAFTTTLNYCVWRDNHGWRGGRRLPE
Target Type
Successful
Target Bioclass
Transporter and channel
Family
TspO/BZRP family
Subcellular location
Mitochondrion membrane
Function
Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme. Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism, but its precise physiological role is controversial. It is apparently not required for steroid hormone biosynthesis. Was initially identified as peripheral-type benzodiazepine receptor; can also bind isoquinoline carboxamides.
TTD ID
T75440
Uniprot ID
P30536
DrugMap ID
TTPTXIN
Ensemble ID
ENST00000329563.8
HGNC ID
HGNC:1158
ChEMBL ID
CHEMBL5742

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A2058 SNV: p.Y65S .
HCT15 SNV: p.L17M .
HT SNV: p.W68R .
SKN SNV: p.V129M .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 17 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C-Sul
 Probe Info 
5.61  LDD0066  [1]
JZ128-DTB
 Probe Info 
N.A.  LDD0462  [2]
THZ1-DTB
 Probe Info 
C19(1.01)  LDD0460  [2]
BTD
 Probe Info 
C19(1.96)  LDD2100  [3]
Jackson_1
 Probe Info 
2.15  LDD0120  [4]
HPAP
 Probe Info 
5.57  LDD0062  [5]
IA-alkyne
 Probe Info 
N.A.  LDD0032  [6]
JW-RF-010
 Probe Info 
N.A.  LDD0026  [7]
NAIA_4
 Probe Info 
N.A.  LDD2226  [8]
TFBX
 Probe Info 
N.A.  LDD0027  [7]
IPM
 Probe Info 
N.A.  LDD0005  [9]
VSF
 Probe Info 
N.A.  LDD0007  [9]
Acrolein
 Probe Info 
C19(0.00); H27(0.00)  LDD0217  [10]
Cinnamaldehyde
 Probe Info 
N.A.  LDD0220  [10]
Crotonaldehyde
 Probe Info 
C19(0.00); H27(0.00)  LDD0219  [10]
Methacrolein
 Probe Info 
N.A.  LDD0218  [10]
NAIA_5
 Probe Info 
N.A.  LDD2223  [8]
PAL-AfBPP Probe
Click To Hide/Show 79 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C004
 Probe Info 
31.12  LDD1714  [11]
C007
 Probe Info 
13.00  LDD1716  [11]
C011
 Probe Info 
7.06  LDD1720  [11]
C017
 Probe Info 
7.46  LDD1725  [11]
C039
 Probe Info 
12.04  LDD1739  [11]
C040
 Probe Info 
11.63  LDD1740  [11]
C044
 Probe Info 
10.27  LDD1743  [11]
C049
 Probe Info 
8.69  LDD1747  [11]
C055
 Probe Info 
39.40  LDD1752  [11]
C056
 Probe Info 
99.73  LDD1753  [11]
C064
 Probe Info 
8.51  LDD1761  [11]
C070
 Probe Info 
15.67  LDD1766  [11]
C072
 Probe Info 
9.45  LDD1768  [11]
C082
 Probe Info 
13.93  LDD1774  [11]
C106
 Probe Info 
18.51  LDD1793  [11]
C107
 Probe Info 
7.31  LDD1794  [11]
C112
 Probe Info 
67.65  LDD1799  [11]
C144
 Probe Info 
8.28  LDD1826  [11]
C159
 Probe Info 
19.16  LDD1839  [11]
C160
 Probe Info 
7.31  LDD1840  [11]
C161
 Probe Info 
11.79  LDD1841  [11]
C169
 Probe Info 
30.48  LDD1849  [11]
C193
 Probe Info 
5.70  LDD1869  [11]
C197
 Probe Info 
5.82  LDD1873  [11]
C198
 Probe Info 
21.71  LDD1874  [11]
C199
 Probe Info 
5.21  LDD1875  [11]
C201
 Probe Info 
24.42  LDD1877  [11]
C206
 Probe Info 
32.45  LDD1881  [11]
C210
 Probe Info 
76.11  LDD1884  [11]
C211
 Probe Info 
9.38  LDD1885  [11]
C218
 Probe Info 
24.76  LDD1892  [11]
C220
 Probe Info 
12.13  LDD1894  [11]
C231
 Probe Info 
14.42  LDD1904  [11]
C232
 Probe Info 
38.05  LDD1905  [11]
C233
 Probe Info 
14.62  LDD1906  [11]
C234
 Probe Info 
19.56  LDD1907  [11]
C235
 Probe Info 
25.46  LDD1908  [11]
C244
 Probe Info 
30.48  LDD1917  [11]
C258
 Probe Info 
5.58  LDD1931  [11]
C262
 Probe Info 
5.94  LDD1934  [11]
C264
 Probe Info 
21.86  LDD1935  [11]
C265
 Probe Info 
13.36  LDD1936  [11]
C266
 Probe Info 
8.75  LDD1937  [11]
C280
 Probe Info 
17.88  LDD1950  [11]
C282
 Probe Info 
16.11  LDD1952  [11]
C285
 Probe Info 
22.16  LDD1955  [11]
C286
 Probe Info 
6.45  LDD1956  [11]
C287
 Probe Info 
8.75  LDD1957  [11]
C289
 Probe Info 
32.22  LDD1959  [11]
C290
 Probe Info 
10.20  LDD1960  [11]
C314
 Probe Info 
18.38  LDD1981  [11]
C317
 Probe Info 
9.92  LDD1983  [11]
C346
 Probe Info 
14.12  LDD2007  [11]
C350
 Probe Info 
33.13  LDD2011  [11]
C354
 Probe Info 
11.79  LDD2015  [11]
C355
 Probe Info 
28.25  LDD2016  [11]
C360
 Probe Info 
4.96  LDD2021  [11]
C361
 Probe Info 
27.86  LDD2022  [11]
C362
 Probe Info 
33.59  LDD2023  [11]
C366
 Probe Info 
10.41  LDD2027  [11]
C373
 Probe Info 
11.96  LDD2033  [11]
C380
 Probe Info 
9.32  LDD2039  [11]
C382
 Probe Info 
23.26  LDD2041  [11]
C388
 Probe Info 
44.32  LDD2047  [11]
C390
 Probe Info 
23.10  LDD2049  [11]
C396
 Probe Info 
7.73  LDD2055  [11]
C403
 Probe Info 
14.42  LDD2061  [11]
C407
 Probe Info 
14.42  LDD2064  [11]
C409
 Probe Info 
5.17  LDD2066  [11]
C413
 Probe Info 
83.29  LDD2069  [11]
C419
 Probe Info 
10.63  LDD2074  [11]
C426
 Probe Info 
60.13  LDD2081  [11]
C428
 Probe Info 
34.78  LDD2083  [11]
C429
 Probe Info 
32.67  LDD2084  [11]
C430
 Probe Info 
5.90  LDD2085  [11]
C431
 Probe Info 
24.25  LDD2086  [11]
C433
 Probe Info 
5.82  LDD2088  [11]
DFG-out-4
 Probe Info 
21.10  LDD0075  [12]
OEA-DA
 Probe Info 
8.31  LDD0046  [13]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C19(1.07)  LDD2112  [3]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C19(0.75)  LDD2117  [3]
 LDCM0108  Chloroacetamide HeLa C19(0.00); H27(0.00)  LDD0222  [10]
 LDCM0070  Cisar_cp37 MDA-MB-231 2.15  LDD0120  [4]
 LDCM0017  DFG-out-2 A431 21.10  LDD0075  [12]
 LDCM0625  F8 Ramos C19(1.33)  LDD2187  [14]
 LDCM0572  Fragment10 Ramos C19(3.60)  LDD2189  [14]
 LDCM0573  Fragment11 Ramos C19(1.00)  LDD2190  [14]
 LDCM0574  Fragment12 Ramos C19(3.03)  LDD2191  [14]
 LDCM0575  Fragment13 Ramos C19(1.07)  LDD2192  [14]
 LDCM0576  Fragment14 Ramos C19(20.00)  LDD2193  [14]
 LDCM0579  Fragment20 Ramos C19(3.07)  LDD2194  [14]
 LDCM0580  Fragment21 Ramos C19(0.68)  LDD2195  [14]
 LDCM0582  Fragment23 Ramos C19(0.65)  LDD2196  [14]
 LDCM0578  Fragment27 Ramos C19(0.52)  LDD2197  [14]
 LDCM0586  Fragment28 Ramos C19(1.22)  LDD2198  [14]
 LDCM0588  Fragment30 Ramos C19(1.53)  LDD2199  [14]
 LDCM0589  Fragment31 Ramos C19(1.18)  LDD2200  [14]
 LDCM0590  Fragment32 Ramos C19(2.29)  LDD2201  [14]
 LDCM0468  Fragment33 Ramos C19(1.11)  LDD2202  [14]
 LDCM0596  Fragment38 Ramos C19(0.33)  LDD2203  [14]
 LDCM0566  Fragment4 Ramos C19(3.42)  LDD2184  [14]
 LDCM0610  Fragment52 Ramos C19(4.62)  LDD2204  [14]
 LDCM0614  Fragment56 Ramos C19(1.98)  LDD2205  [14]
 LDCM0569  Fragment7 Ramos C19(6.65)  LDD2186  [14]
 LDCM0571  Fragment9 Ramos C19(5.55)  LDD2188  [14]
 LDCM0150  Hoch_cp18 MCF-7 C19(3.26)  LDD0380  [15]
 LDCM0107  IAA HeLa C19(0.00); H27(0.00)  LDD0221  [10]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [2]
 LDCM0022  KB02 Ramos C19(20.00)  LDD2182  [14]
 LDCM0023  KB03 MDA-MB-231 C19(0.76)  LDD1701  [3]
 LDCM0024  KB05 Ramos C19(2.37)  LDD2185  [14]
 LDCM0109  NEM HeLa N.A.  LDD0223  [10]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C19(1.96)  LDD2100  [3]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C19(0.74)  LDD2106  [3]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C19(0.82)  LDD2114  [3]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C19(4.79)  LDD2118  [3]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C19(0.85)  LDD2123  [3]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C19(1.22)  LDD2124  [3]
 LDCM0627  NUDT7-COV-1 HEK-293T C19(0.26)  LDD2206  [16]
 LDCM0628  OTUB2-COV-1 HEK-293T C19(1.12)  LDD2207  [16]
 LDCM0014  Panhematin HEK-293T 5.57  LDD0062  [5]
 LDCM0021  THZ1 HeLa S3 C19(1.01)  LDD0460  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
LHFPL tetraspan subfamily member 5 protein (LHFPL5) LHFP family Q8TAF8
Potassium voltage-gated channel subfamily F member 1 (KCNF1) Potassium channel family Q9H3M0
Transmembrane protein 14B (TMEM14B) TMEM14 family Q9NUH8
Proton-transporting V-type ATPase complex assembly regulator TMEM9 (TMEM9) TMEM9 family Q9P0T7
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclic AMP-responsive element-binding protein 3-like protein 1 (CREB3L1) BZIP family Q96BA8
Paired-like homeodomain transcription factor LEUTX (LEUTX) Paired homeobox family A8MZ59
Immunoglobulin
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amphoterin-induced protein 1 (AMIGO1) AMIGO family Q86WK6
Intercellular adhesion molecule 3 (ICAM3) ICAM family P32942
Poliovirus receptor (PVR) Nectin family P15151
Natural cytotoxicity triggering receptor 3 ligand 1 (NCR3LG1) . Q68D85
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein FAM209A (FAM209A) FAM209 family Q5JX71
C-type lectin domain family 10 member A (CLEC10A) . Q8IUN9
Ly6/PLAUR domain-containing protein 5 (LYPD5) . Q6UWN5

The Drug(s) Related To This Target

Approved
Click To Hide/Show 24 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Adinazolam Small molecular drug D0E7FS
Alpidem Small molecular drug D01XOD
Alprazolam Small molecular drug D0L9GG
Chlordiazepoxide Small molecular drug D06BEP
Chlormezanone Small molecular drug D0S1OE
Cinolazepam Small molecular drug D0Q9WO
Clorazepate Small molecular drug D0P3JU
Clotiazepam Small molecular drug D0R4DP
Diazepam Small molecular drug D07JVL
Estazolam Small molecular drug D0P2CK
Eszopiclone Small molecular drug D06ZII
Fludiazepam Small molecular drug D06FWC
Flumazenil Small molecular drug D0D5GD
Flunitrazepam Small molecular drug D0W2NM
Flurazepam Small molecular drug D08XFV
Halazepam Small molecular drug D0Z9VB
Lorazepam Small molecular drug D0E0OG
Midazolam Small molecular drug D0U6LM
Oxazepam Small molecular drug D09LDR
Prazepam Small molecular drug D0G3AQ
Quazepam Small molecular drug D03NPH
Temazepam Small molecular drug D04BNP
Triazolam Small molecular drug D0U3LS
Zopiclone Small molecular drug DB01198
Phase 2
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dextofisopam Small molecular drug D07TXJ
Ssr-180575 Small molecular drug D09OTU
Tln-4601 Small molecular drug D04LTF
11c-pbr-28 . D0G4YZ
Ono-2952 . D05CMZ
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
18f-fedaa-1106 . D0U1US
Bay-85-8102 . D06OFD
Investigative
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(R)Pk-11195 Small molecular drug D0O6JQ
2-(2-phenyl-1h-indol-3-yl)-n,N-dipropyl-acetamide Small molecular drug D0Z4SA
4-methoxy-5-phenyl-6-thia-10b-aza-benzo[E]Azulene Small molecular drug D0M1JT
5-phenyl-6-thia-10b-aza-benzo[E]Azulen-4-one Small molecular drug D08AWL
5-phenyl-6-thia-10b-aza-benzo[E]Azulene Small molecular drug D0A3TE
6-thia-10b-aza-benzo[E]Azulen-4-one Small molecular drug D07WPM
Benzodiazepine Small molecular drug D0CS6N
Fgin-1-27 Small molecular drug D0A0ED
N,N-diethyl-2-(2-phenyl-1h-indol-3-yl)-acetamide Small molecular drug D0T6NJ
N,N-dihexyl-2-(2-phenyl-1h-indol-3-yl)-acetamide Small molecular drug D08XEQ
N,N-dimethyl-2-(2-phenyl-1h-indol-3-yl)-acetamide Small molecular drug D05CYJ
N-hexyl-2-(2-phenyl-1h-indol-3-yl)-acetamide Small molecular drug D0N6IL
Pk 11195 Small molecular drug D0VN4K
Ro 5-4864 Small molecular drug D0B1PE
11c-pbr-170 . D04EGE
Tgsc01aa(4) . D01HGI
U-89854 . D0L2NV
Patented
Click To Hide/Show 93 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aryl Oxyanilide Derivative 1 Small molecular drug D04JEH
Aryl Oxyanilide Derivative 2 Small molecular drug D08RNV
Aryl Oxyanilide Derivative 3 Small molecular drug D0FR9I
Benzimidazolone Acetamide Derivative 1 Small molecular drug D08DPU
Benzimidazolone Acetamide Derivative 2 Small molecular drug D0AC4P
Benzodiazepine Derivative 1 Small molecular drug D0R2XX
Benzothiazepine Analog 1 Small molecular drug D0Z1KU
Benzothiazepine Analog 2 Small molecular drug D08XOA
Benzothiazepine Analog 3 Small molecular drug D03ENW
Benzothiazepine Analog 4 Small molecular drug D0Z6RI
Benzothiazepine Analog 5 Small molecular drug D0GY0E
Benzothiazepine Analog 6 Small molecular drug D05GJL
Benzothiazepine Analog 7 Small molecular drug D0GN5R
Benzothiazepine Analog 8 Small molecular drug D0G7HK
Benzothiazepine Analog 9 Small molecular drug D0O8DG
Benzoxazepine Analog 1 Small molecular drug D0K4VT
Bidentate Pyrazolopyrimidine Acetamide Analog 1 Small molecular drug D0X1MJ
Bidentate Pyrazolopyrimidine Acetamide Analog 2 Small molecular drug D0KZ5O
Bidentate Pyrazolopyrimidine Acetamide Analog 3 Small molecular drug D0G5FS
Bidentate Pyrazolopyrimidine Acetamide Analog 4 Small molecular drug D0X8TY
Imidazopyridine Acetamide Analog 1 Small molecular drug D0PO3M
Imidazopyridine Acetamide Analog 2 Small molecular drug D06PPD
Imidazopyridine Acetamide Analog 3 Small molecular drug D0MR8D
Imidazopyridine Acetamide Analog 4 Small molecular drug D0K4UF
Imidazopyridine Acetamide Analog 5 Small molecular drug D0V9GL
Imidazopyridine Acetamide Analog 6 Small molecular drug D0EG4F
Imidazopyridine Acetamide Analog 7 Small molecular drug D00EBN
Imidazopyridine Derivative 1 Small molecular drug D0HS8T
Imidazopyridine Derivative 2 Small molecular drug D01WQX
Imidazo[1,2-b]Pyridazine Acetamide Derivative 1 Small molecular drug D0M9PB
Imidazo[1,2-b]Pyridazine Acetamide Derivative 2 Small molecular drug D0P1TH
Imidazo[1,2-b]Pyridazine Acetamide Derivative 3 Small molecular drug D08RTY
Imidazo[1,2-b]Pyridazine Acetamide Derivative 4 Small molecular drug D04ESE
Imidazo[1,2-b]Pyridazine Acetamide Derivative 5 Small molecular drug D07RWQ
Imidazo[1,2-b]Pyridazine Acetamide Derivative 6 Small molecular drug D09AKT
Imidazo[1,2-b]Pyridazine Acetamide Derivative 7 Small molecular drug D0K3MV
Indole-based Analog 10 Small molecular drug D01PXI
Indole-based Analog 5 Small molecular drug D00UDJ
Indole-based Analog 9 Small molecular drug D0B3RK
Iodophenyl-n-methyl-n-fluoroalkyl-3-isoquinoline Carboxamide Derivative 1 Small molecular drug D0I6CF
Iodophenyl-n-methyl-n-fluoroalkyl-3-isoquinoline Carboxamide Derivative 2 Small molecular drug D0EY2Q
Iodophenyl-n-methyl-n-fluoroalkyl-3-isoquinoline Carboxamide Derivative 3 Small molecular drug D0CL2E
Isoquinoline Carboxamide Derivative 1 Small molecular drug D01KPW
Phenylpurine Acetamide Analog 1 Small molecular drug D0N5LW
Phenylpurine Acetamide Analog 2 Small molecular drug D0H2RG
Pmid27599163-compound-52 Small molecular drug D0U0IH
Pmid27599163-compound-75 Small molecular drug D0LE6B
Pmid27599163-compound-76 Small molecular drug D07RRL
Pmid27599163-compound-77 Small molecular drug D0JN7L
Pmid27599163-compound-78 Small molecular drug D08ZHA
Pmid27599163-compound-79 Small molecular drug D01DWN
Pmid27599163-compound-81 Small molecular drug D0AP1F
Pmid27599163-compound-82 Small molecular drug D09GSO
Pmid27607364-compound-10 Small molecular drug D0ZK2Q
Pmid27607364-compound-141 Small molecular drug D05ZAV
Pmid27607364-compound-162 Small molecular drug D0RH7L
Pmid27607364-compound-4 Small molecular drug D0N9DS
Pmid27607364-compound-58 Small molecular drug D0A5RG
Pmid27607364-compound-59 Small molecular drug D0E2XN
Pmid27607364-compound-60 Small molecular drug D06HIJ
Pmid27607364-compound-61 Small molecular drug D0TB2L
Pmid27607364-compound-62 Small molecular drug D0IY5H
Pmid27607364-compound-63 Small molecular drug D0Y2ZS
Pmid27607364-compound-64 Small molecular drug D03PTY
Pmid27607364-compound-65 Small molecular drug D01BXA
Pyrazolopyrimidine Acetamide Analog 1 Small molecular drug D01LOJ
Pyrazolopyrimidine Acetamide Analog 2 Small molecular drug D0LB3J
Quinazoline Derivative 2 Small molecular drug D06RNU
Quinazoline Derivative 3 Small molecular drug D09JTT
Quinazoline Derivative 4 Small molecular drug D0S2SS
Quinazoline Derivative 5 Small molecular drug D02UMS
Quinazoline Derivative 6 Small molecular drug D0K3ZB
Quinazoline Derivative 7 Small molecular drug D0TP7S
Quinoline Carboxamide Derivative 10 Small molecular drug D0Y0FR
Quinoline Carboxamide Derivative 4 Small molecular drug D0FF5C
Quinoline Carboxamide Derivative 5 Small molecular drug D0PE1K
Quinoline Carboxamide Derivative 6 Small molecular drug D0OB0Q
Quinoline Carboxamide Derivative 7 Small molecular drug D0AW8P
Quinoline Carboxamide Derivative 8 Small molecular drug D06WUT
Quinoline Carboxamide Derivative 9 Small molecular drug D07KTM
Tricyclic Indole Compound 1 Small molecular drug D0WL7F
Tricyclic Indole Compound 10 Small molecular drug D0RT5D
Tricyclic Indole Compound 11 Small molecular drug D02VRI
Tricyclic Indole Compound 12 Small molecular drug D04SWU
Tricyclic Indole Compound 14 Small molecular drug D0E6TQ
Tricyclic Indole Compound 2 Small molecular drug D0L5EG
Tricyclic Indole Compound 3 Small molecular drug D0R0OA
Tricyclic Indole Compound 4 Small molecular drug D0TQ8V
Tricyclic Indole Compound 5 Small molecular drug D0NF3Y
Tricyclic Indole Compound 6 Small molecular drug D0K3QX
Tricyclic Indole Compound 7 Small molecular drug D0EI2Q
Tricyclic Indole Compound 8 Small molecular drug D0XB2O
Tricyclic Indole Compound 9 Small molecular drug D0Q5JO
Discontinued
Click To Hide/Show 11 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Daa-1097 Small molecular drug D0K5IQ
Emapunil Small molecular drug D05UXF
Ginkgolide B (Gkb) Small molecular drug D03XPV
Imepitoin Small molecular drug D06BYS
Lirequinil Small molecular drug D0O0DF
Miltirone Small molecular drug D02UOE
Ro-16-6028 Small molecular drug D0B3LP
S-8510 Small molecular drug D00TNC
Tro-40303 Small molecular drug D0D5ZR
Nnc-13-8119 . D0Y6LO
Ns-2979 . D0S8KE

References

1 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
2 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
5 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
6 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
7 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
8 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
9 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
10 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
11 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
12 Affinity-based probes based on type II kinase inhibitors. J Am Chem Soc. 2012 Nov 21;134(46):19017-25. doi: 10.1021/ja306035v. Epub 2012 Nov 6.
13 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570
14 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
15 Combined Omics Approach Identifies Gambogic Acid and Related Xanthones as Covalent Inhibitors of the Serine Palmitoyltransferase Complex. Cell Chem Biol. 2020 May 21;27(5):586-597.e12. doi: 10.1016/j.chembiol.2020.03.008. Epub 2020 Apr 23.
16 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.