General Information of the Protein
Protein ID
PT01216
Protein Name
Apoptosis regulator Bcl-2
Gene Name
BCL2
Sequence
MAHAGRTGYDNREIVMKYIHYKLSQRGYEWDAGDVGAAPPGAAPAPGIFSSQPGHTPHPAASRDPVARTSPLQTPAAPGAAAGPALSPVPPVVHLTLRQAGDDFSRRYRRDFAEMSSQLHLTPFTARGRFATVVEELFRDGVNWGRIVAFFEFGGVMCVESVNREMSPLVDNIALWMTEYLNRHLHTWIQDNGGWDAFVELYGPSMRPLFDFSWLSLKTLLSLALVGACITLGAYLGHK
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Other ion channel
>
Miscellaneous ion channel
>
Bcl-2 family
Function
Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells (PubMed:1508712, PubMed:8183370). Regulates cell death by controlling the mitochondrial membrane permeability (PubMed:11368354). Appears to function in a feedback loop system with caspases (PubMed:11368354). Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating factor (APAF-1) (PubMed:11368354). Also acts as an inhibitor of autophagy: interacts with BECN1 and AMBRA1 during non-starvation conditions and inhibits their autophagy function (PubMed:18570871, PubMed:21358617, PubMed:20889974). May attenuate inflammation by impairing NLRP1-inflammasome activation, hence CASP1 activation and IL1B release (PubMed:17418785).
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Uniprot ID
Primary ID:
P10415

Secondarily ID:
C9JHD5
P10416
Q13842
Q16197
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Ensembl ID
ENSG00000171791
HGNC ID
HGNC:990
Subcellular Location
Mitochondrion outer membrane
Nucleus membrane
Endoplasmic reticulum membrane
Cytoplasm
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000121 , FDC-P1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0112166
 Compound Info 
4-[4-[[2-(4-chlorophenyl)-6-[2-(dimethylamino)ethoxy]phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C49H56ClF3N6O7S3
  1
1
IC50 = 4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0281357
 Compound Info 
4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C45H47ClF3N5O6S3
  1
1
IC50 = 14 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0068147
 Compound Info 
(R)-4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-(4-morpholino-1-(phenylthio)butan-2-ylamino)-3-(trifluoromethylsulfonyl)phenylsulfonyl)benzamide
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C47H55ClF3N5O6S3
  1
1
IC50 < 15 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0116815
 Compound Info 
4-[4-[[2-(4-chlorophenyl)-5-[2-(dimethylamino)ethoxy]phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C49H56ClF3N6O7S3
  1
1
IC50 = 22 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0311689
 Compound Info 
4-[4-[[2-(4-chlorophenyl)-6-[2-(dimethylamino)-2-oxoethoxy]phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C49H54ClF3N6O8S3
  1
1
IC50 = 45 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0115928
 Compound Info 
4-[4-[[2-(4-chlorophenyl)-5-[2-(dimethylamino)-2-oxoethoxy]phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C49H54ClF3N6O8S3
  1
1
IC50 = 187 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0054087
 Compound Info 
2-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylpyrimidine-5-carboxamide
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C43H45ClF3N7O6S3
  1
1
IC50 = 340 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0264536
 Compound Info 
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]sulfinyl]piperidin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C45H46ClF3N4O7S4
  1
1
IC50 = 434 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0115927
 Compound Info 
4-[4-[[2-(4-chlorophenyl)phenyl]methyl]-4-cyanopiperidin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C47H47ClF3N5O6S3
  1
1
IC50 = 545 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000001 , Jurkat
 Cell Line Info 
Cell Line ID: CL000048 , PC-3
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0023982
 Compound Info 
4-(4-{[2-(4-chlorophenyl)phenyl]methyl}piperazin-1-yl)-N-[(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzene)sulfonyl]benzamide
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C42H45ClN6O5S2
  13
1 EC50 < 30 nM
2 IC50 < 1 nM
3 IC50 = 6.1 nM
4 IC50 = 7 nM
5 IC50 = 20 nM
6 Kd = 0.6 nM
7 Ki < 1 nM
8 Ki <= 1 nM
9 Ki = 1 nM
10 Ki = 8 nM
11 Ki < 40 nM
12 Ki = 120 nM
13 Ki = 283 nM
CP0112166
 Compound Info 
4-[4-[[2-(4-chlorophenyl)-6-[2-(dimethylamino)ethoxy]phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C49H56ClF3N6O7S3
  1
1 IC50 < 10 nM
CP0115927
 Compound Info 
4-[4-[[2-(4-chlorophenyl)phenyl]methyl]-4-cyanopiperidin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C47H47ClF3N5O6S3
  1
1 IC50 < 10 nM
CP0115928
 Compound Info 
4-[4-[[2-(4-chlorophenyl)-5-[2-(dimethylamino)-2-oxoethoxy]phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C49H54ClF3N6O8S3
  1
1 IC50 < 10 nM
CP0116815
 Compound Info 
4-[4-[[2-(4-chlorophenyl)-5-[2-(dimethylamino)ethoxy]phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C49H56ClF3N6O7S3
  1
1 IC50 < 10 nM
CP0311689
 Compound Info 
4-[4-[[2-(4-chlorophenyl)-6-[2-(dimethylamino)-2-oxoethoxy]phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C49H54ClF3N6O8S3
  1
1 IC50 < 10 nM
CP0068147
 Compound Info 
(R)-4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)-N-(4-(4-morpholino-1-(phenylthio)butan-2-ylamino)-3-(trifluoromethylsulfonyl)phenylsulfonyl)benzamide
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C47H55ClF3N5O6S3
  6
1 IC50 = 10.3 nM
2 Ki < 0.01 nM
3 Ki = 0.044 nM
4 Ki < 0.1 nM
5 Ki < 0.5 nM
6 Ki < 1 nM
CP0281357
 Compound Info 
4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C45H47ClF3N5O6S3
  1
1 IC50 = 11 nM
CP0054087
 Compound Info 
2-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylpyrimidine-5-carboxamide
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C43H45ClF3N7O6S3
  1
1 IC50 = 18 nM
CP0264536
 Compound Info 
4-[4-[(R)-[2-(4-chlorophenyl)phenyl]sulfinyl]piperidin-1-yl]-N-[4-[[(2R)-4-morpholin-4-yl-1-phenylsulfanylbutan-2-yl]amino]-3-(trifluoromethylsulfonyl)phenyl]sulfonylbenzamide
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C45H46ClF3N4O7S4
  1
1 IC50 = 19 nM
CP0096121
 Compound Info 
(N-[(2-tert-butylbenzenesulfonyl)phenyl]-2,3,4-trihydroxy-5-(2-isopropylbenzyl)benzamide
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C33H35NO6S
  3
1 IC50 = 700 nM
2 Ki = 290 nM
3 Ki < 300 nM
CP0146344
 Compound Info 
N-[4-(benzenesulfonyl)phenyl]-5-benzyl-2,3,4-trihydroxybenzamide
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C26H21NO6S
  2
1 IC50 = 1600 nM
2 Ki = 930 nM
CP0044990
 Compound Info 
5-benzyl-2,3,4-trihydroxy-N-phenylbenzamide
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C20H17NO4
  2
1 IC50 = 7200 nM
2 Ki = 8300 nM
CP0160278
 Compound Info 
2,3,4-trihydroxy-5-isopropyl-N-phenyl-benzamide
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C16H17NO4
  3
1 IC50 = 53100 nM
2 Ki = 24100 nM
3 Ki = 31900 nM
CP0088892
 Compound Info 
N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonyl-4-(4,4-dimethylpiperidin-1-yl)benzamide
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C32H41N5O5S2
  2
1 Ki = 62 nM
2 Ki = 67 nM
CP0369570
 Compound Info 
N-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trimethoxy-5-[(2-propan-2-ylphenyl)methyl]benzamide
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C36H41NO6S
  1
1 Ki = 25000 nM
Clinical Information about the Protein
Target 1 ( Apoptosis regulator Bcl-2 (BCL-2) )
Target Type Successful Target
Disease 6 Target-related Diseases  6
1 Chronic lymphocytic leukaemia [ICD-11: 2A82.0]
2 Amyotrophic lateral sclerosis [ICD-11: 8B60.0]
3 Polycystic ovarian syndrome [ICD-11: 5A80.1]
4 Myelofibrosis [ICD-11: 2A20.2]
5 Prostate cancer [ICD-11: 2C82.0]
6 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s) 3 Approved Drugs  3
1 GDC-0199
 Drug Info 
Approved
Chronic lymphocytic leukaemia
2 MCI-186
 Drug Info 
Approved
Amyotrophic lateral sclerosis
3 Taxol
 Drug Info 
Approved
Solid tumour/cancer
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 Thymoquinone
 Drug Info 
Phase 2/3
Polycystic ovarian syndrome
2 ABT-263
 Drug Info 
Phase 3
Myelofibrosis
3 Gossypol
 Drug Info 
Phase 2
Prostate cancer
Investigative Drug(s) 1 Investigative Drug  1
1 Apogossypol
 Drug Info 
Investigative
Solid tumour/cancer
Target 2 ( BCL-2 messenger RNA (BCL2 mRNA) )
Target Type Clinical trial Target