ChEMBL ligand: CHEMBL4173075
endothelial PAS domain protein 1/Endothelial PAS domain-containing protein 1 in Human [ChEMBL: CHEMBL1744522] [GtoPdb: 3148] [UniProtKB: Q99814] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
endothelial PAS domain protein 1/Endothelial PAS domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1744522] [GtoPdb: 3148] [UniProtKB: Q99814]
GtoPdb	Binding affinity for the PAS-B domain of hHIF1α determined by ITC	-	7.3	pKd	50	nM	Kd	Cancer Res (2016) 76: 5491-500 [PMID:27635045]
ChEMBL	Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assay	B	7.92	pIC50	12	nM	IC50	J Med Chem (2018) 61: 9691-9721 [PMID:30289716]
ChEMBL	Inhibition of N-(3-Chlorophenyl-4,6-t2)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine binding to his-tagged HIF-2alpha PAS-B domain (unknown origin) measured after 1 hr by scintillation proximity assay	B	7.92	pIC50	12	nM	IC50	J Med Chem (2019) 62: 6876-6893 [PMID:31282155]
ChEMBL	Antagonist activity at HIF-2alpha in human 786-O cells assessed as free plasma adjusted EC50 for reduction in VEGFA concentration after 24 hrs by ELISA	B	6.8	pEC50	158	nM	EC50	J Med Chem (2018) 61: 9691-9721 [PMID:30289716]
ChEMBL	Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells assessed as reduction in VEGFA level incubated for 20 hrs prior to compound compound washout followed by supplementation of growth medium and subsequent compound addition and measured after 24 hrs by ELISA	B	7.34	pEC50	46	nM	EC50	J Med Chem (2019) 62: 6876-6893 [PMID:31282155]
ChEMBL	Antagonist activity at HIF-2alpha in human 786-O cells assessed as reduction in VEGFA concentration after 24 hrs by ELISA	B	7.39	pEC50	41	nM	EC50	J Med Chem (2018) 61: 9691-9721 [PMID:30289716]
ChEMBL	Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay	B	7.57	pEC50	27	nM	EC50	J Med Chem (2018) 61: 9691-9721 [PMID:30289716]
ChEMBL	Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay	B	7.57	pEC50	27	nM	EC50	J Med Chem (2019) 62: 6876-6893 [PMID:31282155]

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]