danuglipron [Ligand Id: 12064] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4518483 (Danuglipron, Pf-06882961, PF-06882961) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220] | ||||||||
| GtoPdb | Binding affinity of danuglipron evaluated in a competition binding assay with radiolabeled GLP-1 as tracer | - | 6.44 | pKi | 360 | nM | Ki | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Displacement of [125I]GLP-1 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assay | B | 6.44 | pKi | 360 | nM | Ki | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Displacement of [3H]PF-06883365 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assay | B | 7.1 | pKi | 80 | nM | Ki | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Partial agonist activity at N-terminal HA-tagged human GLP-1R expressed in HEK293 cells co-expressing Smbit-beta-arrestin 1/2 and GLP-1R-LgBit assessed as beta-arrestin-1 recruitment measured after 5 mins by bioluminescence based NanoBiT assay | F | 5.69 | pEC50 | 2043 | nM | EC50 | J Med Chem (2023) 66: 7988-8010 [PMID:37286364] |
| ChEMBL | Partial agonist activity at N-terminal HA-tagged human GLP-1R expressed in HEK293 cells co-expressing Smbit-beta-arrestin 1/2 and GLP-1R-LgBit assessed as beta-arrestin-2 recruitment measured after 5 mins by bioluminescence based NanoBiT assay | F | 5.79 | pEC50 | 1614 | nM | EC50 | J Med Chem (2023) 66: 7988-8010 [PMID:37286364] |
| ChEMBL | Agonist activity at N-terminal HA-tagged human GLP-1R expressed in HEK293 cells assessed as change in intracellular calcium level by Fluo-4 AM dye based calcium mobilization assay | F | 5.79 | pEC50 | 1610 | nM | EC50 | J Med Chem (2023) 66: 7988-8010 [PMID:37286364] |
| ChEMBL | Agonist activity at human GLP-1R expressed in PathHunter CHO-K1 GLP1R beta-arrestin-1 cell assessed as induction of beta-arrestin 1 recruitment incubated for 90 mins by pathHunter assay | F | 6.12 | pEC50 | 760 | nM | EC50 | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Agonist activity at human GLP-1R expressed in PathHunter CHO-K1 GLP1R beta-arrestin-2 cell assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by pathHunter assay | F | 6.31 | pEC50 | 490 | nM | EC50 | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Agonist activity at FAP-tagged human GLP-1R expressed in HEK293 cells assessed as receptor internalization | F | 6.64 | pEC50 | 230 | nM | EC50 | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Displacement of [125I]-GLP1 from GLP-1 receptor (unknown origin) expressed in CHO cells membrane pre-incubated for 10 mins followed by [125I]-GLP1 addition and measured after 180 mins by microbeta scintillation counting method | B | 7.89 | pEC50 | 13 | nM | EC50 | Bioorg Med Chem Lett (2023) 94: 129454-129454 [PMID:37591316] |
| ChEMBL | Agonist activity at GLP-1R (unknown origin) expressed in candidate selection CHO cells assessed as cAMP accumulation incubated for 30 mins by plate reader method | F | 7.89 | pEC50 | 13 | nM | EC50 | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Displacement of [125I]GLP-1 from human GLP-1R (7 to 36 residues) expressed in HEK293 or CHO cell membranes after 120 mins by radioligand binding assay | B | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| ChEMBL | Agonist activity at human GLP-1R expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins in absence of BETP by plate reader method | F | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Agonist activity at GLP-1 receptor (unknown origin) expressed in CHO cells by cAMP assay | F | 8.96 | pEC50 | 1.1 | nM | EC50 | Bioorg Med Chem Lett (2023) 94: 129454-129454 [PMID:37591316] |
| ChEMBL | Agonist activity at human GLP-1R expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins in presence of BETP by BETP sensitized time-resolved fluorescence assay | F | 9.15 | pEC50 | 0.71 | nM | EC50 | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| ChEMBL | Agonist activity at N-terminal HA-tagged human GLP-1R expressed in HEK293 cells assessed as effect on intracellular cAMP accumulation incubated for 30 mins by LANCA ultra cAMP assay | F | 10.4 | pEC50 | 0.04 | nM | EC50 | J Med Chem (2023) 66: 7988-8010 [PMID:37286364] |
| GLP-1 receptor/Glucagon-like peptide 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075290] [GtoPdb: 249] [UniProtKB: O35659] | ||||||||
| ChEMBL | Activation of mouse GLP-1R expressed in CHO cells assessed as increase in cAMP accumulation | F | 4.7 | pEC50 | >20000 | nM | EC50 | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| GLP-1 receptor/Glucagon-like peptide 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5862] [GtoPdb: 249] [UniProtKB: P32301] | ||||||||
| ChEMBL | Activation of rat GLP-1R expressed in CHO cells assessed as increase in cAMP accumulation | F | 4.7 | pEC50 | >20000 | nM | EC50 | J Med Chem (2022) 65: 8208-8226 [PMID:35647711] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of hERG | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2023) 66: 7988-8010 [PMID:37286364] |
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]
