ChEMBL ligand: CHEMBL3655081 (Abrocitinib, Cibinqo, Pf-04965842, PF-04965842)
Janus kinase 2/Janus kinase 1/tyrosine kinase 2/JAK1/JAK2/TYK2 in Human [ChEMBL: CHEMBL3301390] [GtoPdb: 2048, 2047, 2269] [UniProtKB: O60674, P23458, P29597] There should be some charts here, you may need to enable JavaScript!
Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human [ChEMBL: CHEMBL3301391] [GtoPdb: 2047, 2269] [UniProtKB: P23458, P29597] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/Janus kinase 1/JAK2/JAK1 in Human [ChEMBL: CHEMBL3038492] [GtoPdb: 2048, 2047] [UniProtKB: O60674, P23458] There should be some charts here, you may need to enable JavaScript!
Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human [ChEMBL: CHEMBL3301392] [GtoPdb: 2048, 2269] [UniProtKB: O60674, P29597] There should be some charts here, you may need to enable JavaScript!
Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human [ChEMBL: CHEMBL3038491] [GtoPdb: 2047, 2049] [UniProtKB: P23458, P52333] There should be some charts here, you may need to enable JavaScript!
Monoamine oxidase A in Human [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] There should be some charts here, you may need to enable JavaScript!
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/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] There should be some charts here, you may need to enable JavaScript!
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] There should be some charts here, you may need to enable JavaScript!
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] There should be some charts here, you may need to enable JavaScript!
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] 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 2/Janus kinase 1/tyrosine kinase 2/JAK1/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301390] [GtoPdb: 2048, 2047, 2269] [UniProtKB: O60674, P23458, P29597]
GtoPdb	-	-	6.1	pIC50	803	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK1/JAK2/TYK2 in CD14+ human whole blood assessed as reduction in IL-6 induced STAT1 phosphorylation preincubated for 45 mins followed by IL-6 addition measured after 15 mins by flow cytometric analysis	B	6.79	pIC50	163	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
GtoPdb	-	-	7.54	pIC50	29	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301391] [GtoPdb: 2047, 2269] [UniProtKB: P23458, P29597]
ChEMBL	Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IL-10 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-10 addition measured after 15 mins by flow cytometric analysis	B	5.6	pIC50	2511	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK1/TYK2 in human M07E cells assessed as reduction of IFN alpha stimulated STAT phosphorylation preincubated for 30 mins followed by IFN alpha stimulation and measured after 15 mins by flow cytometry method	B	6.55	pIC50	284	nM	IC50	J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL	Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFNalpha induced STAT3 phosphorylation preincubated for 45 mins followed by IFNalpha addition measured after 15 mins by flow cytometric analysis	B	6.72	pIC50	189	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
GtoPdb	-	-	7.54	pIC50	29	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
Janus kinase 2/Janus kinase 1/JAK2/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038492] [GtoPdb: 2048, 2047] [UniProtKB: O60674, P23458]
GtoPdb	-	-	6.1	pIC50	803	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK2/JAK1 in human whole blood assessed as reduction in IL-27 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-27 addition measured after 15 mins by flow cytometric analysis	B	6.57	pIC50	271	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK2/JAK1 in human whole blood assessed as reduction in IFNgamma induced STAT1 phosphorylation preincubated for 45 mins followed by IFNgamma addition measured after 15 mins by flow cytometric analysis	B	6.79	pIC50	163	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
GtoPdb	-	-	7.54	pIC50	29	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301392] [GtoPdb: 2048, 2269] [UniProtKB: O60674, P29597]
ChEMBL	Inhibition of JAK2/TYK2 in human whole blood assessed as reduction in IL-23 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-23 addition measured after 15 mins by flow cytometric analysis	B	4.78	pIC50	>16452	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK2/TYK2 in human whole blood assessed as reduction in IL-12 induced STAT4 phosphorylation preincubated for 45 mins followed by IL-12 addition measured after 15 mins by flow cytometric analysis	B	4.86	pIC50	13673	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
GtoPdb	-	-	6.1	pIC50	803	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038491] [GtoPdb: 2047, 2049] [UniProtKB: P23458, P52333]
ChEMBL	Inhibition of JAK1/JAK3 in CD8+ human whole blood assessed as reduction in IL-15 induced STAT5 phosphorylation preincubated for 45 mins followed by IL-15 addition measured after 15 mins by flow cytometric analysis	B	5.89	pIC50	1298	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK1/JAK3 in human whole blood assessed as reduction in IL-21 induced STAT3 phosphorylation preincubated for 45 mins followed by IL-21 addition measured after 15 mins by flow cytometric analysis	B	6.29	pIC50	511	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK1/JAK3 in human blood assessed as reduction of IL-2 stimulated STAT phosphorylation preincubated for 30 mins followed by IL-2 stimulation and measured after 15 mins by flow cytometry method	B	7.05	pIC50	90	nM	IC50	J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL	Inhibition of JAK1/JAK3 in human M07E cells assessed as reduction of IL-15 stimulated STAT phosphorylation preincubated for 30 mins followed by IL-15 stimulation and measured after 15 mins by flow cytometry analysis	B	7.33	pIC50	47	nM	IC50	J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
GtoPdb	-	-	7.54	pIC50	29	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL	Inhibition of MAOA (unknown origin)	B	5.22	pIC50	6000	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL	Inhibition of JAK1 in human STAT6-bla-RA1 cells assessed as reduction in IL4-induced STAT6-signalling pre-incubated for 1 hrs before human recombinant IL4 addition and further incubated for 4 hrs fluorescence based assay	B	6.74	pIC50	180	nM	IC50	J Med Chem (2020) 63: 7008-7032 [PMID:32462873]
ChEMBL	Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4.	B	7.54	pIC50	29	nM	IC50	US-9035074-B2. Pyrrolo[2,3-D]pyrimidine derivatives (2015)
ChEMBL	Inhibition of recombinant human JAK1 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assay	B	7.54	pIC50	29	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK 1 (unknown origin)	B	7.54	pIC50	29	nM	IC50	J Med Chem (2022) 65: 893-921 [PMID:33539089]
GtoPdb	-	-	7.54	pIC50	29	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK1 JH1 domain (unknown origin) using FITC-Ahx-KKSRGDYMTMQIG-NH2 peptide as substrate incubated for 60 mins in the presence of ATP by caliper microfluidic mobility shift technology	B	7.7	pIC50	20	nM	IC50	J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL	Inhibition of N-terminal GST-tagged human JAK1 catalytic domain (850 to 1154 residues) incubated for 40 mins in presence of TK substrate-biotin by TR-FRET assay	B	8.29	pIC50	5.1	nM	IC50	J Med Chem (2020) 63: 7008-7032 [PMID:32462873]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL	Inhibition of JAK2 in human STAT5-irf1-bla TF1 cells assessed as reduction in EPO-induced STAT5-signalling pre-incubated for 1 hrs before EPO addition and further incubated for 4 hrs fluorescence based assay	B	5.85	pIC50	1400	nM	IC50	J Med Chem (2020) 63: 7008-7032 [PMID:32462873]
ChEMBL	Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4.	B	6.1	pIC50	803	nM	IC50	US-9035074-B2. Pyrrolo[2,3-D]pyrimidine derivatives (2015)
GtoPdb	-	-	6.1	pIC50	803	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK2 JH1 domain (unknown origin) using Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK peptide as substrate incubated for 60 mins in the presence of ATP by caliper microfluidic mobility shift technology	B	6.39	pIC50	412	nM	IC50	J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL	Inhibition of N-terminal His-tagged human JAK2 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay	B	7.44	pIC50	36	nM	IC50	J Med Chem (2020) 63: 7008-7032 [PMID:32462873]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL	Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4.	B	5	pIC50	>10000	nM	IC50	US-9035074-B2. Pyrrolo[2,3-D]pyrimidine derivatives (2015)
ChEMBL	Inhibition of recombinant human JAK3 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of JAK3 JH1 domain (unknown origin) using Carboxyfluorescein-Ahx-GGEEEEYFELVKKKK peptide as substrate incubated for 60 mins in the presence of ATP by caliper microfluidic mobility shift technology	B	5.15	pIC50	7073	nM	IC50	J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL	Inhibition of recombinant human JAK3 using FITC-KGGEEEEYFELVKK as substrate in presence of 4 uM ATP by mobility shift assay	B	6.22	pIC50	605	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]
ChEMBL	Inhibition of N-terminal His-tagged human JAK3 catalytic domain incubated for 20 mins in presence of TK substrate-biotin by TR-FRET assay	B	6.32	pIC50	480	nM	IC50	J Med Chem (2020) 63: 7008-7032 [PMID:32462873]
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL	Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4.	B	5.9	pIC50	1250	nM	IC50	US-9035074-B2. Pyrrolo[2,3-D]pyrimidine derivatives (2015)
ChEMBL	Inhibition of TYK2 (unknown origin) by caliper technology	B	6.26	pIC50	549	nM	IC50	J Med Chem (2023) 66: 2161-2168 [PMID:36657024]
ChEMBL	Inhibition of N-terminal GST-tagged human TYK2 catalytic domain (871 to 1187 residues) incubated for 40 mins in presence of TK substrate-biotin by TR-FRET assay	B	6.8	pIC50	160	nM	IC50	J Med Chem (2020) 63: 7008-7032 [PMID:32462873]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL	Inhibition of recombinant human VEGFR2 expressed in Sf9 cells	B	5.92	pIC50	1200	nM	IC50	J Med Chem (2018) 61: 1130-1152 [PMID:29298069]

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]