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 | Binding affinity to ERR-gamma LBD (unknown origin) assessed as dissociation constant by ITC analysis | B | 4.87 | pKd | 13600 | nM | Kd | Eur J Med Chem (2023) 250: 115174-115174 [PMID:36805944] |
| 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] |
| ChEMBL | Inverse agonist activity at Gal4-tagged mouse ERR-gamma LBD transfected in HEK293T cells co-expressing FR-luc assessed as inhibition of transcriptional activity incubated for 24 hrs by luciferase reporter gene assay | B | 8.1 | pIC50 | 7.92 | nM | IC50 | Eur J Med Chem (2023) 250: 115174-115174 [PMID:36805944] |
| 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 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]
