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] |
| ChEMBL | Inhibition of C-terminal His6-tagged Bcl-2 (1 to 212 residues) (unknown origin) expressed in Escherichia coli using biotin-labeled Bim peptide GGMRPEIWIANELRRIGDEFNA as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2021) 32: 127717-127717 [PMID:33253879] |
| Bcl-2-like 2/Apoptosis regulator Bcl-W in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4677] [GtoPdb: 2846] [UniProtKB: Q92843] | ||||||||
| ChEMBL | Inhibition of N-terminal His6-tagged Bcl-w (1 to 171 residues) (unknown origin) expressed in Escherichia coli using biotin-labeled Bim peptide GGMRPEIWIANELRRIGDEFNA as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 7.7 | pIC50 | >20 | nM | IC50 | Bioorg Med Chem Lett (2021) 32: 127717-127717 [PMID:33253879] |
| 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] |
| ChEMBL | Inhibition of N-terminal GST-tagged Bcl-xL (1 to 209 residues) (unknown origin) expressed in Escherichia coli using fFluor 647-labeled BAK peptide GGGQVGRQLAIIGDDINR as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2021) 32: 127717-127717 [PMID:33253879] |
| Bcl-2-related protein A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6044] [UniProtKB: Q16548] | ||||||||
| ChEMBL | Inhibition of N-terminal His6-tagged Bfl-1 (1 to 151 residues) (unknown origin) expressed in Escherichia coli using Fluor 647-labeled BAK peptide WIAQELRRIGDEFN as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 7.7 | pIC50 | >20 | nM | IC50 | Bioorg Med Chem Lett (2021) 32: 127717-127717 [PMID:33253879] |
| 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] |
| ChEMBL | Inhibition of N-terminal GST-tagged Mcl-1 (171 to 327 residues) (unknown origin) expressed in Escherichia coli using fluor 647-labeled Bim peptide WIAQELRRIGDEFN as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 9.7 | pKi | 0.2 | nM | Ki | Bioorg Med Chem Lett (2021) 32: 127717-127717 [PMID:33253879] |
| ChEMBL | Displacement of Fluor 647-labeled BIM peptide from N-terminal GST-tagged MCL-1 (unknown origin) assessed as inhibition constant incubated for 120 to 180 mins by TR-FRET assay | B | 9.7 | pKi | 0.2 | nM | Ki | ACS Med Chem Lett (2023) 14: 955-961 [PMID:37465311] |
| 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 | Inhibition of N-terminal GST-tagged Mcl-1 (171 to 327 residues) (unknown origin) expressed in Escherichia coli using fluor 647-labeled Bim peptide WIAQELRRIGDEFN as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Bioorg Med Chem Lett (2021) 32: 127717-127717 [PMID:33253879] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
