Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T61683 | Target Info | |||
| Target Name | Inhibitor of apoptosis protein (hIAP) | ||||
| Synonyms |
Baculoviral IAP repeat-containing protein
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| Target Type | Clinical trial Target | ||||
| Gene Name | XIAP; BIRC2; BIRC3; NAIP; BIRC5; BIRC7 | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Cellular inhibitor of apoptosis 1 (BIRC2) | Clinical trial Target | ||||
| UniProt ID | BIRC2_HUMAN | |||||
| Gene Name | BIRC2 | |||||
| Synonyms |
hIAP2; hIAP-2; TNFR2TRAFsignaling complex protein 2; TNFR2-TRAF-signaling complex protein 2; RNF48; RING-type E3 ubiquitin transferase BIRC2; RING finger protein 48; MIHB; Inhibitor of apoptosis protein 2; IAP2; IAP homolog B; CIAP1; C-IAP1; Baculoviral IAP repeatcontaining protein 2; Baculoviral IAP repeat-containing protein 2; API1
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| Representative Drug(s) | LCL161 | Drug Info | EC50 = 0.4 nM | Click to Show More | [1] | |
| 2 | AT-406 | Drug Info | Ki = 1.9 nM | [2] | ||
| Co-Target Name | Cellular inhibitor of apoptosis 2 (BIRC3) | Clinical trial Target | ||||
| UniProt ID | BIRC3_HUMAN | |||||
| Gene Name | BIRC3 | |||||
| Synonyms |
hIAP1; hIAP-1; TNFR2TRAFsignaling complex protein 1; TNFR2-TRAF-signaling complex protein 1; RNF49; RING-type E3 ubiquitin transferase BIRC3; RING finger protein 49; MIHC; Inhibitor of apoptosis protein 1; IAP1; IAP homolog C; CIAP2; C-IAP2; Baculoviral IAP repeatcontaining protein3; Baculoviral IAP repeat-containing protein 3; Apoptosis inhibitor 2; API2
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| Representative Drug(s) | AT-406 | Drug Info | Ki = 5.1 nM | Click to Show More | [2] | |
| 2 | LCL161 | Drug Info | IC50 = 11 nM | [3] | ||
| Co-Target Name | X-linked inhibitor of apoptosis protein (XIAP) | Clinical trial Target | ||||
| UniProt ID | XIAP_HUMAN | |||||
| Gene Name | XIAP | |||||
| Synonyms |
hILP; hIAP3; hIAP-3; Xlinked IAP; X-linked IAP; RING-type E3 ubiquitin transferase XIAP; Inhibitor of apoptosis protein 3; ILP; IAPlike protein; IAP3; IAP-like protein; IAP-3; E3 ubiquitinprotein ligase XIAP; E3 ubiquitin-protein ligase XIAP; Baculoviral IAP repeatcontaining protein 4; Baculoviral IAP repeat-containing protein 4; BIRC4; API3
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| Representative Drug(s) | LCL161 | Drug Info | IC50 = 30 nM | Click to Show More | [4] | |
| 2 | AT-406 | Drug Info | EC50 = 34 nM | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP). J Med Chem. 2017 Jun 8;60(11):4611-25. | ||||
| REF 2 | A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment. J Med Chem. 2011 Apr 28;54(8):2714-26. | ||||
| REF 3 | Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy. J Med Chem. 2019 Oct 24;62(20):9188-9200. | ||||
| REF 4 | Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain. J Med Chem. 2013 Oct 24;56(20):7788-803. | ||||
| REF 5 | Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP. J Med Chem. 2015 Aug 27;58(16):6574-88. | ||||
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