GSK5182 [Ligand Id: 8908] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL201013 (GSK5182)
  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • Estrogen-related receptor-β/Estrogen-related receptor beta in Human [ChEMBL: CHEMBL3751] [GtoPdb: 623] [UniProtKB: O95718]
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  • Estrogen-related receptor-γ/Estrogen-related receptor gamma in Human [ChEMBL: CHEMBL4245] [GtoPdb: 624] [UniProtKB: P62508]
  • Estrogen-related receptor-γ/Estrogen-related receptor gamma in Mouse [ChEMBL: CHEMBL3585238] [GtoPdb: 624] [UniProtKB: P62509]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
GtoPdb - - 6.49 pIC50 320 nM IC50 Bioorg Med Chem Lett (2006) 16: 821-4 [PMID:16307879]
ChEMBL Displacement of [3H]estradiol from ERalpha B 6.49 pIC50 320 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 821-824 [PMID:16307879]
Estrogen-related receptor-β/Estrogen-related receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3751] [GtoPdb: 623] [UniProtKB: O95718]
ChEMBL Inverse agonist activity at GAL4-DNA binding domain-fused human ERRbeta ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay B 5.46 pIC50 3500 nM IC50 Bioorg Med Chem (2017) 25: 1585-1599 [PMID:28189393]
Estrogen-related receptor-γ/Estrogen-related receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4245] [GtoPdb: 624] [UniProtKB: P62508]
ChEMBL Inhibition of interaction between ERRgamma and NR cofactor RIP140 in FRET assay F 6.6 pIC50 250 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 821-824 [PMID:16307879]
GtoPdb - - 7.1 pIC50 79 nM IC50 Bioorg Med Chem Lett (2006) 16: 821-4 [PMID:16307879]
ChEMBL Displacement of [3H]4-OHT from ERRgamma B 7.1 pIC50 79 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 821-824 [PMID:16307879]
Estrogen-related receptor-γ/Estrogen-related receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3585238] [GtoPdb: 624] [UniProtKB: P62509]
ChEMBL Inverse agonist activity at GAL4-DNA binding domain-fused mouse ERRgamma ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay B 5.57 pIC50 2700 nM IC50 Bioorg Med Chem (2017) 25: 1585-1599 [PMID:28189393]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]