Any inhibitor of B-cell lymphoma 2 protein.
ChEBI ID: 133022
| Member | Definition | Class |
|---|---|---|
| abt-199 | A member of the class of pyrrolopyridines that is a potent inhibitor of the antiapoptotic protein B-cell lymphoma 2. It is used for treamtment of chronic lymphocytic leukemia with 17p deletion. | venetoclax |
| abt-737 | A biphenyl that is 4-chloro-1,1'-biphenyl substituted by a (4-{4-[(4-{[(2R)-4-(dimethylamino)-1-(phenylsulfanyl)butan-2-yl]amino}-3-nitrobenzene-1-sulfonyl)carbamoyl]phenyl}piperazin-1-yl)methyl group at position 2'. It is a BH3-mimetic drug which targets the anti-apoptotic B-cell lymphoma-2 (BCL-2) family proteins, including BCL-2, BCL-xL, and BCL-w, and induces apoptosis in cancer cells. | ABT-737 |
| navitoclax | A N-sulfonylcarboxamide resulting from the formal condensation of the carboxy group of 4-{4-[(4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro[biphenyl]-2-yl)methyl]piperazin-1-yl}benzoic acid with the amino group of 4-{[(2R)-4-(morpholin-4-yl)-1-(phenylsulfanyl)butan-2-yl]amino}-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide. It is a BH3-mimetic drug which targets the anti-apoptotic B-cell lymphoma-2 (BCL-2) family proteins, including BCL-2, BCL-xL, and BCL-w, and induces apoptosis in cancer cells. Currently under clinical investigation as treatment for solid tumors and hematologic malignancies. | navitoclax |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 109 (4.58) | 29.6817 |
| 2010's | 1,110 (46.66) | 24.3611 |
| 2020's | 1,160 (48.76) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 165 (6.49%) | 5.53% |
| Reviews | 317 (12.46%) | 6.00% |
| Case Studies | 135 (5.31%) | 4.05% |
| Observational | 4 (0.16%) | 0.25% |
| Other | 1,923 (75.59%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 67.9K protein | Vaccinia virus | Potency | 10.6101 | 2 | 2 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 95.2834 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 53.4132 | 2 | 2 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 35.6740 | 2 | 2 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 17.9734 | 4 | 12 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| Interferon beta | Homo sapiens (human) | Potency | 16.5388 | 1 | 3 |
| PPM1D protein | Homo sapiens (human) | Potency | 16.5388 | 1 | 2 |
| Smad3 | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 1.5849 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 0.3814 | 2 | 2 |
| tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 30.7475 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Adenosine receptor A2a | Rattus norvegicus (Norway rat) | IC50 | 0.0200 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0003 | 1 | 1 |
| Alpha-2A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0003 | 1 | 1 |
| Alpha-2B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0003 | 1 | 1 |
| Alpha-2C adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0003 | 1 | 1 |
| Apoptosis regulator BAX | Homo sapiens (human) | IC50 | 0.0230 | 1 | 1 |
| Apoptosis regulator Bcl-2 | Homo sapiens (human) | IC50 | 0.5443 | 18 | 25 |
| Apoptosis regulator Bcl-2 | Homo sapiens (human) | Ki | 0.0102 | 36 | 42 |
| Aspartyl/asparaginyl beta-hydroxylase | Homo sapiens (human) | IC50 | 1.9925 | 4 | 12 |
| Bcl-2 homologous antagonist/killer | Homo sapiens (human) | IC50 | 16.6890 | 3 | 3 |
| Bcl-2 homologous antagonist/killer | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| Bcl-2-binding component 3, isoforms 1/2 | Homo sapiens (human) | IC50 | 0.0003 | 1 | 1 |
| Bcl-2-like protein 1 | Homo sapiens (human) | IC50 | 0.6990 | 26 | 34 |
| Bcl-2-like protein 1 | Homo sapiens (human) | Ki | 0.0519 | 47 | 51 |
| Bcl-2-like protein 10 | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| Bcl-2-like protein 11 | Homo sapiens (human) | IC50 | 0.0032 | 2 | 2 |
| Bcl-2-like protein 2 | Homo sapiens (human) | IC50 | 1.2839 | 5 | 8 |
| Bcl-2-like protein 2 | Homo sapiens (human) | Ki | 0.1280 | 8 | 8 |
| Bcl-2-related protein A1 | Homo sapiens (human) | IC50 | 0.7511 | 1 | 4 |
| Bcl-2-related protein A1 | Homo sapiens (human) | Ki | 20.0000 | 1 | 1 |
| Bcl2-associated agonist of cell death | Homo sapiens (human) | Ki | 3.2006 | 4 | 5 |
| Beta-casein | Bos taurus (cattle) | Ki | 0.0010 | 1 | 1 |
| BH3-interacting domain death agonist | Homo sapiens (human) | IC50 | 16.5242 | 2 | 2 |
| BH3-interacting domain death agonist | Homo sapiens (human) | Ki | 20.8000 | 1 | 1 |
| Chain A, Apoptosis regulator Bcl-X | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| Induced myeloid leukemia cell differentiation protein Mcl-1 | Homo sapiens (human) | IC50 | 8.5057 | 11 | 18 |
| Induced myeloid leukemia cell differentiation protein Mcl-1 | Homo sapiens (human) | Ki | 26.9659 | 15 | 15 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Apoptosis regulator Bcl-2 | Homo sapiens (human) | EC50 | 0.1348 | 11 | 11 |
| Apoptosis regulator Bcl-2 | Homo sapiens (human) | Kd | 0.4222 | 4 | 6 |
| Bcl-2 homologous antagonist/killer | Homo sapiens (human) | EC50 | 0.0200 | 1 | 1 |
| Bcl-2-like protein 1 | Homo sapiens (human) | EC50 | 0.0233 | 3 | 3 |
| Bcl-2-like protein 1 | Homo sapiens (human) | Kd | 0.0009 | 3 | 3 |
| Bcl-2-related protein A1 | Homo sapiens (human) | Kd | 1.0000 | 1 | 1 |
| Induced myeloid leukemia cell differentiation protein Mcl-1 homolog | Mus musculus (house mouse) | Kd | 1.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Chain A, BCL-2-RELATED PROTEIN A1 | Homo sapiens (human) | AbsAC10_uM | 3.0900 | 1 | 1 |