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 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]