AZD5991 [Ligand Id: 11783] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4297482 (Azd 5991, Azd-5991, Azd5991, AZD-5991, AZD5991) |
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| 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 | Inhibition of Fluor 647-labeled Bim peptide C binding to human C-Terminal 6His-tagged Bcl-2 expressed in Escherichia coli incubated for 120 to 180 mins by lanthascreen TR-FRET assay | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2021) 64: 10260-10285 [PMID:34228434] |
| Bcl-2-like 1/Apoptosis regulator Bcl-X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817] | ||||||||
| ChEMBL | Inhibition of Fluor 647-labeled Bim peptide C binding to human N-terminal GST-tagged Bcl-xL expressed in Escherichia coli incubated for 120 to 180 mins by lanthascreen TR-FRET assay | B | 4.44 | pIC50 | 36000 | nM | IC50 | J Med Chem (2021) 64: 10260-10285 [PMID:34228434] |
| 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 FITC-labeled Bak BH3 peptide binding to GST-tagged MCL1 (171 to 327 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 30 mins fluorescence polarization-based competitive binding assay | B | 9 | pKi | <1 | nM | Ki | J Med Chem (2021) 64: 11330-11353 [PMID:34342996] |
| ChEMBL | Inhibition of N-terminal GST-tagged-Mcl1 (E171 to G327) (unknown origin) expressed in Escherichia coli using HyLite Fluor 647-labeled Bim peptide C as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2020) 63: 928-943 [PMID:31580668] |
| GtoPdb | - | - | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2020) 63: 928-943 [PMID:31580668] |
| ChEMBL | Inhibition of N-terminal GST-tagged MCl-1 (unknown origin) expressed in Escherichia coli cells after 120 to 180 mins by TR-FRET-binding affinity assay | B | 9.77 | pKi | 0.17 | nM | Ki | Eur J Med Chem (2019) 177: 63-75 [PMID:31129454] |
| ChEMBL | Inhibition of Fluor 647-labeled Bim peptide C binding to human N-terminal GST-tagged-Mcl-1 expressed in Escherichia coli incubated for 120 to 180 mins by lanthascreen TR-FRET assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2021) 64: 10260-10285 [PMID:34228434] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
