Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 13:18:53 GMT 2023
by
admin
on
Sat Dec 16 13:18:53 GMT 2023
|
| Protein Type | REGULATOR PROTEIN |
| Protein Sub Type | ANTI-APOPTOCTIC REGULATORY PROTEIN |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
8RQM3E2NEV
|
| Record Status |
Validated (UNII)
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| Record Version |
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-
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Common Name | English |
| Code System | Code | Type | Description | ||
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P10415
Created by
admin on Sat Dec 16 13:18:55 GMT 2023 , Edited by admin on Sat Dec 16 13:18:55 GMT 2023
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PRIMARY | |||
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8RQM3E2NEV
Created by
admin on Sat Dec 16 13:18:55 GMT 2023 , Edited by admin on Sat Dec 16 13:18:55 GMT 2023
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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INHIBITOR -> TARGET |
Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 3.
IC50
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
S55746 occupies the hydrophobic groove of BCL-2. Its selectivity profile demonstrates no significant binding to MCL-1, BFL-1 (BCL2A1/A1) and poor affinity for BCL-XL. Accordingly, S55746 has no cytotoxic activity on BCL-XL-dependent cells, such as platelets.
Ki
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2.
IC50
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INHIBITOR -> TARGET |
TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.
IC50
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET |
Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.
IC50
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INHIBITOR -> TARGET |
Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.
ANTAGONIST
IC50
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INHIBITOR -> TARGET |
Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively
INHIBITOR
IC50
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INHIBITOR -> TARGET |
Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.
POTENT
IC50
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INHIBITOR -> TARGET |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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