JAK3 inhibitor II [Ligand Id: 5993] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL473773 (WHI-P154)
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • epidermal growth factor receptor in Human [GtoPdb: 1797] [UniProtKB: P00533]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of ABCG2 (unknown origin) expressed in MDCK2 cells co-expressing BCRP (unknown origin) assessed as potentiation of SN-38-induced cytotoxicity measured after 72 hrs by MTT assay B 6.72 pEC50 189 nM EC50 Eur J Med Chem (2019) 164: 193-213 [PMID:30594677]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of ABCB1 in human A2780/ADR cells assessed as potentiation of daunorubicin-induced cytotoxicity measured after 72 hrs by MTT assay B 5.51 pEC50 3080 nM EC50 Eur J Med Chem (2019) 164: 193-213 [PMID:30594677]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
GtoPdb - - 5 pIC50 >10000 nM IC50 Blood (2008) 111: 2155-7 [PMID:18094329]
ChEMBL Inhibition of JAK1 B 5 pIC50 >10000 nM IC50 Science (2003) 302: 875-878 [PMID:14593182]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
GtoPdb - - 5 pIC50 >10000 nM IC50 Blood (2008) 111: 2155-7 [PMID:18094329]
ChEMBL Inhibition of JAK2 B 5 pIC50 >10000 nM IC50 Science (2003) 302: 875-878 [PMID:14593182]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
GtoPdb - - 5.74 pIC50 1800 nM IC50 Blood (2008) 111: 2155-7 [PMID:18094329]
ChEMBL Inhibition of JAK3 (unknown origin) B 5.74 pIC50 1800 nM IC50 J Med Chem (2018) 61: 9811-9840 [PMID:29969256]
epidermal growth factor receptor in Human [GtoPdb: 1797] [UniProtKB: P00533]
GtoPdb - - 8.4 pIC50 4 nM IC50 Blood (2008) 111: 2155-7 [PMID:18094329]

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]