Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T56510 | Target Info | |||
| Target Name | Apoptosis regulator Bcl-xL (BCL-xL) | ||||
| Synonyms |
Bcl2like protein 1; Bcl2L1; Bcl2-L-1; Bcl-XL; Bcl-2-like protein 1; BCLX; BCL2L; Apoptosis regulator Bcl-X
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| Target Type | Clinical trial Target | ||||
| Gene Name | BCL2L1 | ||||
| Biochemical Class | B-cell lymphoma Bcl-2 | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Apoptosis regulator Bcl-2 (BCL-2) | Successful Target | ||||
| UniProt ID | BCL2_HUMAN | |||||
| Gene Name | BCL2 | |||||
| Synonyms |
Bcl-2
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| Representative Drug(s) | ABT-263 | Drug Info | Ki < 0.01 nM | Click to Show More | [1] | |
| 2 | Obatoclax | Drug Info | EC50 = 300 nM | [2] | ||
| Co-Target Name | Induced myeloid leukemia cell differentiation protein Mcl-1 (MCL1) | Clinical trial Target | ||||
| UniProt ID | MCL1_HUMAN | |||||
| Gene Name | MCL1 | |||||
| Synonyms |
mcl1/EAT; Bcl2-L-3; Bcl-2-related protein EAT/mcl1; Bcl-2-like protein 3; BCL2L3
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| Representative Drug(s) | ABT-263 | Drug Info | Ki < 1 nM | Click to Show More | [3] | |
| 2 | Obatoclax | Drug Info | EC50 = 500 nM | [2] | ||
| Co-Target Name | Apoptosis regulator Bcl-W (BCL-W) | Clinical trial Target | ||||
| UniProt ID | B2CL2_HUMAN | |||||
| Gene Name | BCL2L2 | |||||
| Synonyms |
KIAA0271; Bcl2-L-2; Bcl-2-like protein 2; BCLW
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| Representative Drug(s) | ABT-263 | Drug Info | IC50 = 70 nM | Click to Show More | [4] | |
| 2 | Obatoclax | Drug Info | Ki = 1000 nM | [5] | ||
| Co-Target Name | Bcl-2-related protein A1 (BCL2A1) | Patented-recorded Target | ||||
| UniProt ID | B2LA1_HUMAN | |||||
| Gene Name | BCL2A1 | |||||
| Synonyms |
Protein GRS; Protein BFL-1; Hemopoietic-specific early response protein; HBPA1; GRS; Bcl2-L-5; Bcl-2-like protein 5; BFL1; BCL2L5
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| Representative Drug(s) | Obatoclax | Drug Info | EC50 = 600 nM | [2] | ||
| Co-Target Name | Bcl2-antagonist of cell death (BAD) | Co-Target | ||||
| UniProt ID | BAD_HUMAN | |||||
| Gene Name | BAD | |||||
| Synonyms |
Bcl2-associated agonist of cell death; BAD; Bcl-2-binding component 6; Bcl-2-like protein 8; Bcl2-L-8; Bcl-xL/Bcl-2-associated death promoter; Bcl2 antagonist of cell death
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| Representative Drug(s) | ABT-263 | Drug Info | Ki < 0.5 nM | Click to Show More | [6] | |
| 2 | Obatoclax | Drug Info | Ki = 1000 nM | [5] | ||
| Co-Target Name | Bcl-2-like protein 10 (BCL2L10) | Co-Target | ||||
| UniProt ID | B2L10_HUMAN | |||||
| Gene Name | BCL2L10 | |||||
| Synonyms |
Bcl2-L-10; Anti-apoptotic protein NrH; Apoptosis regulator Bcl-B
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| Representative Drug(s) | Obatoclax | Drug Info | Ki = 1000 nM | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Clinical candidates modulating protein-protein interactions: The fragment-based experience. Eur J Med Chem. 2019 Apr 1;167:76-95. | ||||
| REF 2 | Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators. Eur J Med Chem. 2012 Nov;57:112-25. | ||||
| REF 3 | The chemical biology of apoptosis: Revisited after 17 years. Eur J Med Chem. 2019 Sep 1;177:63-75. | ||||
| REF 4 | Discovery and optimization of covalent Bcl-xL antagonists. Bioorg Med Chem Lett. 2019 Dec 1;29(23):126682. | ||||
| REF 5 | Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. | ||||
| REF 6 | Recent developments in fragment-based drug discovery. J Med Chem. 2008 Jul 10;51(13):3661-80. | ||||
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