GR 159897 [Ligand Id: 2115] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2110370 (GR-159897)
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  • GLP-1 receptor/Glucagon-like peptide 1 receptor in Human [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
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  • GPR119/Glucose-dependent insulinotropic receptor in Human [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5]
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  • FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
  • NK2 receptor/Neurokinin 2 receptor in Rat [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: APLNR F 5 pIC50 >10000 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: GLP1R F 5.12 pEC50 7501.09 nM EC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
GPR119/Glucose-dependent insulinotropic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR119 F 5 pIC50 >10000 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4 F 5 pIC50 >10000 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
GtoPdb - - 9.5 pKd - - - Biochem Biophys Res Commun (1993) 191: 1172-7 [PMID:7682062];
J Med Chem (1995) 38: 3772-9 [PMID:7562907];
Eur J Pharmacol (1995) 272: 241-8 [PMID:7713168]
ChEMBL Binding affinity against Tachykinin receptor 2 of human expressed in chinese hamster ovary cells B 9.5 pKi 0.32 nM Ki Bioorg Med Chem Lett (1994) 4: 1951-1956
NK2 receptor/Neurokinin 2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4554] [GtoPdb: 361] [UniProtKB: P16610]
ChEMBL Binding affinity by displacement of radiolabeled GR-100679 from Tachykinin receptor 2 from homogenized rat colon B 10 pKi 0.1 nM Ki Bioorg Med Chem Lett (1994) 4: 1951-1956
Neurokinin 3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3799] [UniProtKB: P30098]
ChEMBL Tested for inhibition of binding of [3H]senktide to Tachykinin receptor 3 in guinea pig cerebral cortex membranes B 4.7 pKi 19952.62 nM Ki Bioorg Med Chem Lett (1994) 4: 1951-1956

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]