ChEMBL ligand: CHEMBL3137309 (ABT-199, GDC-0199, RG-7601, RG7601, Venclexta, Venclyxto, Venetoclax)
BCL2 apoptosis regulator/Apoptosis regulator Bcl-2 in Human [ChEMBL: CHEMBL4860] [GtoPdb: 2844] [UniProtKB: P10415] There should be some charts here, you may need to enable JavaScript!
Bcl-2-like 2/Apoptosis regulator Bcl-W in Human [ChEMBL: CHEMBL4677] [GtoPdb: 2846] [UniProtKB: Q92843] There should be some charts here, you may need to enable JavaScript!
Bcl-2-like 1/Apoptosis regulator Bcl-X in Human [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817] There should be some charts here, you may need to enable JavaScript!
Aspartyl/asparaginyl beta-hydroxylase in Human [ChEMBL: CHEMBL4680030] [UniProtKB: Q12797] There should be some charts here, you may need to enable JavaScript!
Bcl2-antagonist of cell death (BAD) in Human [ChEMBL: CHEMBL3817] [UniProtKB: Q92934] There should be some charts here, you may need to enable JavaScript!
MCL1 apoptosis regulator, BCL2 family member/Induced myeloid leukemia cell differentiation protein Mcl-1 in Human [ChEMBL: CHEMBL4361] [GtoPdb: 2847] [UniProtKB: Q07820] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
BCL2 apoptosis regulator/Apoptosis regulator Bcl-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4860] [GtoPdb: 2844] [UniProtKB: P10415]
ChEMBL	Binding affinity to human full-length N-terminal His6-tagged prephosphorylated Bcl2 (2 to 206 residues) expressed in Escherichia coli S12 extract by isothermal titration calorimetry	B	6.15	pKd	705	nM	Kd	J Med Chem (2020) 63: 13733-13744 [PMID:33197310]
ChEMBL	Binding affinity to human full-length N-terminal His6-tagged Bcl2 (2 to 206 residues) expressed in Escherichia coli S12 extract by isothermal titration calorimetry	B	8.51	pKd	3.1	nM	Kd	J Med Chem (2020) 63: 13733-13744 [PMID:33197310]
ChEMBL	Binding affinity to recombinant Bcl-2 D103V mutant (unknown origin) using peptide probe incubated for 2 hrs by fluorescence based assay	B	7.23	pKi	59	nM	Ki	Eur J Med Chem (2022) 232: 114184-114184 [PMID:35182816]
ChEMBL	Binding affinity to recombinant Bcl-2 D103E mutant (unknown origin) using peptide probe incubated for 2 hrs by fluorescence based assay	B	7.77	pKi	17	nM	Ki	Eur J Med Chem (2022) 232: 114184-114184 [PMID:35182816]
ChEMBL	Binding affinity to recombinant wild-type Bcl-2 (unknown origin) using peptide probe incubated for 2 hrs by fluorescence based assay	B	8.92	pKi	1.2	nM	Ki	Eur J Med Chem (2022) 232: 114184-114184 [PMID:35182816]
ChEMBL	Inhibition of FAM-Bid binding to human BCL2 expressed in Escherichia coli BL21 after 30 mins by fluorescence polarization assay	B	9	pKi	<1	nM	Ki	ACS Med Chem Lett (2016) 7: 1185-1190 [PMID:27994761]
ChEMBL	Binding affinity to full length human Bcl-2 expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant preincubated for 30 mins followed by 5-FAM-QEDIIIINIARHLAQVGDSMD-RSIPPG tracer addition and measured after 20 mins by fluorescence polarization assay	B	9	pKi	<1	nM	Ki	J Med Chem (2021) 64: 10260-10285 [PMID:34228434]
ChEMBL	Binding affinity to BCL2 (unknown origin) incubated for 30 mins by TR-FRET assay	B	10	pKi	<0.1	nM	Ki	Medchemcomm (2016) 7: 778-787
ChEMBL	Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) Assay: The inhibition constant (Ki) is the dissociation constant of an enzyme-inhibitor complex or a protein/small molecule complex, wherein the small molecule is inhibiting binding of one protein to another protein or peptide. Where the Ki for a compound is represented as > (greater than) a certain numerical value, it is intended to mean that the binding affinity value (e.g., for Bcl-XL) is greater than the limits of detection of the assay used. Where the binding selectivity ratio for a compound is represented as > (greater than) a certain numerical value, it is intended to mean that the selectivity of a particular compound for Bcl-2 over Bcl-XL is at least as great as the number indicated. Where the Ki for a compound is represented as < (less than) a certain numerical value, it is intended to mean that the binding affinity value (e.g., for Bcl-2) is lower than the limit of detection of the assay used. Inhibition constants were determined using Wang's equation (Wang Z-X).	B	10.44	pKi	0.04	nM	Ki	US-9125913-B2. Bcl-2-selective apoptosis-inducing agents for the treatment of cancer and immune diseases (2015)
ChEMBL	Inhibition of wild-type BCL-2 (unknown origin) expressed in Escherichia coli BL21 cells using biotinylated BIMBH3 or BAXBH3 peptide by surface plasmon resonance assay	B	10.74	pKi	0.02	nM	Ki	J Med Chem (2020) 63: 928-943 [PMID:31580668]
GtoPdb	Note that this Ki is below the detection limit of the assay.	-	11	pKi	<0.01	nM	Ki	US8580794. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases. (2013); Nat Med (2013) 19: 202-8 [PMID:23291630]
ChEMBL	Displacement of fluorescent-labeled BID-BH3 peptide from human BCL-2 expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant by fluorescence polarization-based competitive binding assay	B	11	pKi	<0.01	nM	Ki	Eur J Med Chem (2022) 236: 114327-114327 [PMID:35385805]
ChEMBL	Binding affinity to Bcl-2 (unknown origin) by FRET assay	B	11	pKi	<0.01	nM	Ki	Bioorg Med Chem Lett (2016) 26: 2105-2114 [PMID:26988306]
ChEMBL	Binding affinity to Bcl-2 (unknown origin) assessed as inhibition constant by TR-FRET assay	B	11	pKi	<0.01	nM	Ki	Eur J Med Chem (2020) 201: 112446-112446 [PMID:32563811]
ChEMBL	Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Representative compounds were serially diluted in dimethyl sulfoxide (DMSO) starting at 50 uM (2x starting concentration; 10% DMSO) and 10 uL were transferred into a 384-well plate. Then 10 uL of a protein/probe/antibody mix was added to each well at final concentrations listed in TABLE 1. Protein:GST-Bcl-2, Probe: F-Bak Peptide Probe Acetyl-GQVGRQLAIIGDK(6-FAM)INR-amide(SEQ ID NO: 1), Protein(nM): 1, Probe (nM): 100, Antibody: Tb-anit-GST, Antibody (nm): 1. The samples are then mixed on a shaker for 1 minute and incubated for an additional 3 hours at room temperature. For each assay, the probe/antibody and protein/probe/antibody were included on each assay plate as negative and positive controls, respectively. Fluorescence was measured on the ENVISION plate reader (Perkin Elmer) using a 340/35 nm excitation filter and 520/525 (F-Bak peptide) and 495/510 nm (Tb-labeled anti-Histidine antibody) emission filters.	B	11	pKi	<0.01	nM	Ki	US-9174982-B2. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases (2015)
ChEMBL	Binding affinity to Bcl-2 (unknown origin) by TR-FRET assay	B	11	pKi	<0.01	nM	Ki	J Med Chem (2017) 60: 821-838 [PMID:27749061]
ChEMBL	Inhibition of Bcl-2 (unknown origin) by TR-FRET assay	B	11	pKi	<0.01	nM	Ki	Eur J Med Chem (2018) 146: 471-482 [PMID:29407973]
ChEMBL	Inhibition of Bcl2 (unknown origin)	B	11	pKi	<0.01	nM	Ki	J Med Chem (2018) 61: 6421-6467 [PMID:29620890]
ChEMBL	Inhibition of Bcl2 (unknown origin)	B	11	pKi	<0.01	nM	Ki	J Med Chem (2018) 61: 2636-2651 [PMID:28926247]
ChEMBL	Inhibition of Bcl2 (unknown origin)	B	11	pKi	<0.01	nM	Ki	Eur J Med Chem (2019) 177: 63-75 [PMID:31129454]
ChEMBL	Inhibition of BCL2 (unknown origin) by TR-FRET assay	B	11	pKi	<0.01	nM	Ki	J Med Chem (2020) 63: 11420-11435 [PMID:32539387]
ChEMBL	Inhibition of FAM-Bid peptide binding to Bcl2 (unknown origin) by fluorescence polarization assay	B	6.64	pIC50	230	nM	IC50	Bioorg Med Chem Lett (2019) 29: 349-352 [PMID:30594434]
ChEMBL	Inhibition of FAM-Bim peptide binding to human Bcl-2 (2 to 206) measured after 30 mins by fluorescence polarization assay	B	7	pIC50	>100	nM	IC50	Eur J Med Chem (2021) 220: 113452-113452 [PMID:33906046]
ChEMBL	Inhibition of BCL-2 (unknown origin)	B	7.64	pIC50	23	nM	IC50	J Med Chem (2021) 64: 1362-1391 [PMID:33523672]
ChEMBL	Inhibition of FAM-labelled Bax binding to Bcl2 (unknown origin) after 30 mins by fluorescence polarization assay	B	8.13	pIC50	7.4	nM	IC50	Eur J Med Chem (2018) 159: 149-165 [PMID:30278333]
ChEMBL	Displacement of Bax-derived peptide from Bcl-2 (unknown origin) by fluorescence polarization assay	B	8.13	pIC50	7.39	nM	IC50	Bioorg Med Chem (2018) 26: 443-454 [PMID:29229225]
ChEMBL	Inhibition of FAM-Bid binding to human BCL2 expressed in Escherichia coli BL21 after 30 mins by fluorescence polarization assay	B	9	pIC50	<1	nM	IC50	ACS Med Chem Lett (2016) 7: 1185-1190 [PMID:27994761]
ChEMBL	Displacement of Bak derived peptide from Bcl-2 (unknown origin) measured after 15 mins by microplate reader assay	B	9	pIC50	1	nM	IC50	Bioorg Med Chem (2021) 47: 116350-116350 [PMID:34536651]
ChEMBL	Inhibition of BCL-2 (unknown origin) by fluorescence polarization assay	B	8.52	pEC50	3	nM	EC50	Eur J Med Chem (2019) 167: 76-95 [PMID:30769242]
Bcl-2-like 2/Apoptosis regulator Bcl-W in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4677] [GtoPdb: 2846] [UniProtKB: Q92843]
GtoPdb	-	-	6.61	pKi	245	nM	Ki	Nat Med (2013) 19: 202-8 [PMID:23291630]
ChEMBL	Binding affinity to Bcl-w (unknown origin) by TR-FRET assay	B	6.61	pKi	245	nM	Ki	J Med Chem (2017) 60: 821-838 [PMID:27749061]
ChEMBL	Displacement of fluorescent-labeled BID-BH3 peptide from human BCL-W expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant by fluorescence polarization-based competitive binding assay	B	6.61	pKi	245	nM	Ki	Eur J Med Chem (2022) 236: 114327-114327 [PMID:35385805]
ChEMBL	Binding affinity to Bcl-w (unknown origin) assessed as inhibition constant by TR-FRET assay	B	6.61	pKi	245	nM	Ki	Eur J Med Chem (2020) 201: 112446-112446 [PMID:32563811]
Bcl-2-like 1/Apoptosis regulator Bcl-X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817]
ChEMBL	Binding affinity to Bcl-xL (unknown origin) assessed as inhibition constant by TR-FRET assay	B	7.32	pKi	48	nM	Ki	Eur J Med Chem (2020) 201: 112446-112446 [PMID:32563811]
ChEMBL	Binding affinity to His-tagged Bcl-XL (unknown origin) incubated for 30 mins by TR-FRET assay	B	7.32	pKi	48	nM	Ki	Medchemcomm (2016) 7: 778-787
ChEMBL	Binding affinity to Bcl-xL (unknown origin) by TR-FRET assay	B	7.32	pKi	48	nM	Ki	J Med Chem (2017) 60: 821-838 [PMID:27749061]
ChEMBL	Inhibition of Bcl-xL (unknown origin) by TR-FRET assay	B	7.32	pKi	48	nM	Ki	Eur J Med Chem (2018) 146: 471-482 [PMID:29407973]
ChEMBL	Inhibition of Bcl-xL (unknown origin)	B	7.32	pKi	48	nM	Ki	J Med Chem (2018) 61: 2636-2651 [PMID:28926247]
ChEMBL	Displacement of fluorescent-labeled BID-BH3 peptide from human BCL-xL expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant by fluorescence polarization-based competitive binding assay	B	7.32	pKi	48	nM	Ki	Eur J Med Chem (2022) 236: 114327-114327 [PMID:35385805]
ChEMBL	Binding affinity to Bcl-XL (unknown origin) by FRET assay	B	7.32	pKi	48	nM	Ki	Bioorg Med Chem Lett (2016) 26: 2105-2114 [PMID:26988306]
GtoPdb	-	-	7.32	pKi	48	nM	Ki	Nat Med (2013) 19: 202-8 [PMID:23291630]
ChEMBL	Binding affinity to Bc1-xL (unknown origin) by fluorescence polarization competition assay	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2021) 47: 128215-128215 [PMID:34153472]
ChEMBL	Binding affinity to full length human Bcl-xl expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant preincubated for 30 mins followed by 5-FAM-QEDIIIINIARHLAQVGDSMD-RSIPPG tracer addition and measured after 20 mins by fluorescence polarization assay	B	9	pKi	<1	nM	Ki	J Med Chem (2021) 64: 10260-10285 [PMID:34228434]
ChEMBL	Displacement of Bak derived peptide from Bcl-xL (unknown origin) measured after 15 mins by microplate reader assay	B	6.8	pIC50	157	nM	IC50	Bioorg Med Chem (2021) 47: 116350-116350 [PMID:34536651]
Aspartyl/asparaginyl beta-hydroxylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4680030] [UniProtKB: Q12797]
ChEMBL	Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using high 10 uM hFX-CP as substrate mixture with 10 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis	B	5.8	pIC50	1570	nM	IC50	Bioorg Med Chem (2020) 28: 115675-115675 [PMID:33069066]
ChEMBL	Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with high 200 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis	B	5.82	pIC50	1520	nM	IC50	Bioorg Med Chem (2020) 28: 115675-115675 [PMID:33069066]
ChEMBL	Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis	B	5.85	pIC50	1400	nM	IC50	Bioorg Med Chem (2020) 28: 115675-115675 [PMID:33069066]
ChEMBL	Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and high 20 uM FAS incubated for 35 mins by MS analysis	B	5.89	pIC50	1290	nM	IC50	Bioorg Med Chem (2020) 28: 115675-115675 [PMID:33069066]
Bcl2-antagonist of cell death (BAD) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3817] [UniProtKB: Q92934]
ChEMBL	Binding affinity to Bcl-2 (unknown origin) by fluorescence polarization competition assay	B	4.8	pKi	16000	nM	Ki	Bioorg Med Chem Lett (2021) 47: 128215-128215 [PMID:34153472]
MCL1 apoptosis regulator, BCL2 family member/Induced myeloid leukemia cell differentiation protein Mcl-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4361] [GtoPdb: 2847] [UniProtKB: Q07820]
ChEMBL	Inhibition of FAM-Bid binding to human MCL1 expressed in Escherichia coli BL21 after 30 mins by fluorescence polarization assay	B	6.11	pKi	>780	nM	Ki	ACS Med Chem Lett (2016) 7: 1185-1190 [PMID:27994761]
GtoPdb	-	-	6.35	pKi	>444	nM	Ki	Nat Med (2013) 19: 202-8 [PMID:23291630]
ChEMBL	Binding affinity to MCL1 (unknown origin) incubated for 30 mins by TR-FRET assay	B	6.35	pKi	>444	nM	Ki	Medchemcomm (2016) 7: 778-787
ChEMBL	Binding affinity to Mcl-1 (unknown origin) by TR-FRET assay	B	6.35	pKi	>444	nM	Ki	J Med Chem (2017) 60: 821-838 [PMID:27749061]
ChEMBL	Inhibition of Mcl-1 (unknown origin) by TR-FRET assay	B	6.35	pKi	>444	nM	Ki	Eur J Med Chem (2018) 146: 471-482 [PMID:29407973]
ChEMBL	Displacement of fluorescent-labeled BID-BH3 peptide from His-tagged human MCL-1 expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant by fluorescence polarization-based competitive binding assay	B	6.35	pKi	>444	nM	Ki	Eur J Med Chem (2022) 236: 114327-114327 [PMID:35385805]
ChEMBL	Binding affinity to Mcl-1 (unknown origin) assessed as inhibition constant by TR-FRET assay	B	6.35	pKi	>444	nM	Ki	Eur J Med Chem (2020) 201: 112446-112446 [PMID:32563811]
ChEMBL	Inhibition of FAM-Bid binding to human MCL1 expressed in Escherichia coli BL21 after 30 mins by fluorescence polarization assay	B	5.4	pIC50	>4000	nM	IC50	ACS Med Chem Lett (2016) 7: 1185-1190 [PMID:27994761]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]