GSK5182 [Ligand Id: 8908] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL201013 (GSK5182) |
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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] | ||||||||
| ChEMBL | Binding affinity to GST-tagged ERalpha LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay | B | 5.59 | pIC50 | 2590 | nM | IC50 | J Med Chem (2016) 59: 10209-10227 [PMID:27805390] |
| ChEMBL | Binding affinity to ERalpha (unknown origin) by TR-FRET assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | Eur J Med Chem (2020) 205: 112501-112501 [PMID:32758860] |
| 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-α/Estrogen-related receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3429] [GtoPdb: 622] [UniProtKB: P11474] | ||||||||
| ChEMBL | Binding affinity to GST-tagged ERRalpha LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 10209-10227 [PMID:27805390] |
| ChEMBL | Binding affinity to ERRalpha (unknown origin) by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2020) 205: 112501-112501 [PMID:32758860] |
| Estrogen-related receptor-β/Estrogen-related receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3751] [GtoPdb: 623] [UniProtKB: O95718] | ||||||||
| ChEMBL | Binding affinity to GST-tagged ERRbeta LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 10209-10227 [PMID:27805390] |
| ChEMBL | Binding affinity to ERRbeta (unknown origin) by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2020) 205: 112501-112501 [PMID:32758860] |
| 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] |
| ChEMBL | Binding affinity to GST-tagged ERRgamma LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2016) 59: 10209-10227 [PMID:27805390] |
| ChEMBL | Binding affinity to ERRgamma (unknown origin) by TR-FRET assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2020) 205: 112501-112501 [PMID:32758860] |
| 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] |
| ChEMBL | Inverse agonist activity at ERRgamma (unknown origin) by luciferase reporter gene assay | B | 7.11 | pIC50 | 77 | nM | IC50 | Eur J Med Chem (2020) 205: 112501-112501 [PMID:32758860] |
| 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] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG measured after 4 hrs by fluorescence polarization assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2016) 59: 10209-10227 [PMID:27805390] |
| ChEMBL | Inhibition of human ERG by fluorescence polarization assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | Eur J Med Chem (2020) 205: 112501-112501 [PMID:32758860] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
