ChEMBL ligand: CHEMBL3301606 (G-154578, G154578, Glpg-0778, GLPG-0778, GLPG0778, GLPG-0788, Gsk-2586184, GSK-2586184, GSK-2586184A, GSK2586184A, Solcitinib)
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2 in Human [GtoPdb: 2048] [UniProtKB: O60674] There should be some charts here, you may need to enable JavaScript!
Janus kinase 3 in Human [GtoPdb: 2049] [UniProtKB: P52333] There should be some charts here, you may need to enable JavaScript!
tyrosine kinase 2 in Human [GtoPdb: 2269] [UniProtKB: P29597] 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
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
GtoPdb	-	-	8.18	pIC50	6.6	nM	IC50	WO2010149771. Novel compound useful for the treatment of degenerative and inflammatory diseases (2010)
ChEMBL	Inhibition Assay: Recombinant human JAK1 (catalytic domain, amino acids 866-1154; catalog number PV4774) was purchased from Invitrogen. 1 ng of JAK1 was incubated with 20 nM Ulight-JAK1(tyr1023) peptide (Perkin Elmer catalog number TRF0121) in kinase reaction buffer (25 mM MOPS pH6.8, 0.016% Brij-35, 8.33 mM MgCl2, 3.33 mM DTT, 7 uM ATP) with or without 4 uL containing test compound or vehicle (DMSO, 1% final concentration), in a total volume of 20 uL, in a white 384 Luminotrac 200 plate (Greiner, catalog number 781075). After 60 min at room temperature, reactions were stopped by adding 20 uL/well of detection mixture (1x detection buffer (Perkin Elmer, catalog number CR97-100C), 0.5 nM Europium-anti-phosphotyrosine (PT66) (Perkin Elmer, catalog number AD0068), 10 mM EDTA). Readout is performed using the Envision with excitation at 320 nm and measuring emission at 615 nm (Perkin Elmer). Kinase activity was calculated by subtracting relative fluorescence units (RFU).	B	8.18	pIC50	6.6	nM	IC50	US-8796457-B2. Compound useful for the treatment of degenerative and inflammatory diseases (2014)
Janus kinase 2 in Human [GtoPdb: 2048] [UniProtKB: O60674]
GtoPdb	-	-	7.17	pIC50	67	nM	IC50	WO2010149771. Novel compound useful for the treatment of degenerative and inflammatory diseases (2010)
Janus kinase 3 in Human [GtoPdb: 2049] [UniProtKB: P52333]
GtoPdb	-	-	6.39	pIC50	408	nM	IC50	WO2010149771. Novel compound useful for the treatment of degenerative and inflammatory diseases (2010)
tyrosine kinase 2 in Human [GtoPdb: 2269] [UniProtKB: P29597]
GtoPdb	-	-	6.66	pIC50	219	nM	IC50	WO2010149771. Novel compound useful for the treatment of degenerative and inflammatory diseases (2010)

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]