solangepras [Ligand Id: 11514] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4778540
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GPR6/G-protein coupled receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714130] [GtoPdb: 85] [UniProtKB: P46095]
ChEMBL Displacement of 3H-RL338 from human GPR6 expressed in T-REx-CHO-GPR6 cells assessed as inhibition constant by competition binding assay B 8.03 pKi 9.4 nM Ki J Med Chem (2021) 64: 9875-9890 [PMID:33861086]
GtoPdb - - 8.03 pKi 9.4 nM Ki J Med Chem (2021) 64: 9875-9890 [PMID:33861086]
ChEMBL Binding affinity to GPR6 (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting based competition binding assay B 8.26 pKi 5.5 nM Ki US-10406157-B2. Tetrahydropyridopyrazine modulators of GPR6 (2019)
ChEMBL Inverse agonist activity at human GPR6 expressed in CHO-K1 cells assessed as modulation of cAMP level incubated for 20 hrs by TR-FRET assay F 4.42 pEC50 38000 nM EC50 J Med Chem (2021) 64: 9875-9890 [PMID:33861086]
ChEMBL Inhibition of GPR6 (unknown origin) expressed in CHO-K1 cells assessed as decrease in constitutive cAMP activity by HTRF assay F 7.2 pEC50 63.1 nM EC50 US-10406157-B2. Tetrahydropyridopyrazine modulators of GPR6 (2019)
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 5.71 pIC50 1970 nM IC50 US-10406157-B2. Tetrahydropyridopyrazine modulators of GPR6 (2019)

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]