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Assay Detail

CHEMBL4022972

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Binding
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
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

JAK1/TYK2 (CHEMBL3301391) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R.
J Med Chem (2018) 61 : 1130 -1152
PubMed 29298069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 6.51 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2105759 BARICITINIB 4.0 1 7.54
CHEMBL221959 TOFACITINIB 4.0 1 7.46
CHEMBL4059667 — — 1 7.05
CHEMBL4103698 — — 1 6.97
CHEMBL3655104 — — 1 6.85
CHEMBL4093955 — — 1 6.83
CHEMBL3655080 — — 1 6.83
CHEMBL4101374 — — 1 6.81
CHEMBL3658860 — — 1 6.81
CHEMBL3655086 — — 1 6.80
CHEMBL4063642 — — 1 6.73
CHEMBL3655081 ABROCITINIB 4.0 1 6.72
CHEMBL1789941 RUXOLITINIB 4.0 1 6.71
CHEMBL4068319 — — 1 6.70
CHEMBL4085264 — — 1 6.68
CHEMBL4104105 — — 1 6.68
CHEMBL3655082 — — 1 6.67
CHEMBL4099048 — — 1 6.67
CHEMBL4087961 — — 1 6.59
CHEMBL3655095 — — 1 6.59
CHEMBL4098094 — — 1 6.48
CHEMBL4079179 — — 1 6.43
CHEMBL4087044 — — 1 6.22
CHEMBL4065613 — — 1 6.20
CHEMBL4066404 — — 1 6.19
CHEMBL4103435 — — 1 6.16
CHEMBL4100048 — — 1 6.14
CHEMBL4100431 — — 1 6.12
CHEMBL3655097 — — 1 6.11
CHEMBL4092805 — — 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2105759 BARICITINIB IC50 = 29.0 nM 7.54
CHEMBL221959 TOFACITINIB IC50 = 35.0 nM 7.46
CHEMBL4059667 — IC50 = 89.0 nM 7.05
CHEMBL4103698 — IC50 = 107.0 nM 6.97
CHEMBL3655104 — IC50 = 141.0 nM 6.85
CHEMBL4093955 — IC50 = 148.0 nM 6.83
CHEMBL3655080 — IC50 = 147.0 nM 6.83
CHEMBL4101374 — IC50 = 156.0 nM 6.81
CHEMBL3658860 — IC50 = 155.0 nM 6.81
CHEMBL3655086 — IC50 = 160.0 nM 6.80
CHEMBL4063642 — IC50 = 186.0 nM 6.73
CHEMBL3655081 ABROCITINIB IC50 = 189.0 nM 6.72
CHEMBL1789941 RUXOLITINIB IC50 = 194.0 nM 6.71
CHEMBL4068319 — IC50 = 199.0 nM 6.70
CHEMBL4104105 — IC50 = 211.0 nM 6.68
CHEMBL4085264 — IC50 = 207.0 nM 6.68
CHEMBL3655082 — IC50 = 212.0 nM 6.67
CHEMBL4099048 — IC50 = 216.0 nM 6.67
CHEMBL4087961 — IC50 = 256.0 nM 6.59
CHEMBL3655095 — IC50 = 259.0 nM 6.59
CHEMBL4098094 — IC50 = 331.0 nM 6.48
CHEMBL4079179 — IC50 = 367.0 nM 6.43
CHEMBL4087044 — IC50 = 601.0 nM 6.22
CHEMBL4065613 — IC50 = 628.0 nM 6.20
CHEMBL4066404 — IC50 = 645.0 nM 6.19
CHEMBL4103435 — IC50 = 692.0 nM 6.16
CHEMBL4100048 — IC50 = 721.0 nM 6.14
CHEMBL4100431 — IC50 = 750.0 nM 6.12
CHEMBL3655097 — IC50 = 773.0 nM 6.11
CHEMBL4092805 — IC50 = 930.0 nM 6.03
CHEMBL4077614 — IC50 = 1189.0 nM 5.92
CHEMBL4090590 — IC50 = 1400.0 nM 5.85
CHEMBL4085011 — IC50 = 2480.0 nM 5.61
CHEMBL4101725 — IC50 = 6450.0 nM 5.19
CHEMBL4078655 — IC50 - — -
CHEMBL4082035 — IC50 - — -
CHEMBL4066876 — IC50 - — -
CHEMBL4071850 — IC50 - — -
CHEMBL4093643 — IC50 - — -
CHEMBL4059894 — IC50 - — -
CHEMBL4089286 — IC50 - — -
CHEMBL4103586 — IC50 - — -
CHEMBL4075575 — IC50 - — -