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Assay Detail

CHEMBL4022969

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant human JAK1 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assay
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK1 (CHEMBL2835) ↗
Type SINGLE PROTEIN
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 7.58 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4103698 — — 1 8.52
CHEMBL2105759 BARICITINIB 4.0 1 8.40
CHEMBL4093955 — — 1 8.30
CHEMBL1789941 RUXOLITINIB 4.0 1 8.22
CHEMBL4101374 — — 1 8.22
CHEMBL4079179 — — 1 8.10
CHEMBL3658860 — — 1 8.05
CHEMBL4068319 — — 1 8.00
CHEMBL4103586 — — 1 8.00
CHEMBL4103435 — — 1 7.96
CHEMBL4066876 — — 1 7.96
CHEMBL4087961 — — 1 7.92
CHEMBL4077614 — — 1 7.85
CHEMBL3655082 — — 1 7.85
CHEMBL221959 TOFACITINIB 4.0 1 7.82
CHEMBL4099048 — — 1 7.82
CHEMBL4063642 — — 1 7.77
CHEMBL4066404 — — 1 7.72
CHEMBL4059894 — — 1 7.72
CHEMBL4104105 — — 1 7.68
CHEMBL3655104 — — 1 7.66
CHEMBL3655080 — — 1 7.66
CHEMBL3655086 — — 1 7.55
CHEMBL3655081 ABROCITINIB 4.0 1 7.54
CHEMBL4093643 — — 1 7.52
CHEMBL4059667 — — 1 7.51
CHEMBL4085264 — — 1 7.44
CHEMBL4087044 — — 1 7.43
CHEMBL4089286 — — 1 7.41
CHEMBL4090590 — — 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4103698 — IC50 = 3.0 nM 8.52
CHEMBL2105759 BARICITINIB IC50 = 4.0 nM 8.40
CHEMBL4093955 — IC50 = 5.0 nM 8.30
CHEMBL1789941 RUXOLITINIB IC50 = 6.0 nM 8.22
CHEMBL4101374 — IC50 = 6.0 nM 8.22
CHEMBL4079179 — IC50 = 8.0 nM 8.10
CHEMBL3658860 — IC50 = 9.0 nM 8.05
CHEMBL4068319 — IC50 = 10.0 nM 8.00
CHEMBL4103586 — IC50 = 10.0 nM 8.00
CHEMBL4103435 — IC50 = 11.0 nM 7.96
CHEMBL4066876 — IC50 = 11.0 nM 7.96
CHEMBL4087961 — IC50 = 12.0 nM 7.92
CHEMBL4077614 — IC50 = 14.0 nM 7.85
CHEMBL3655082 — IC50 = 14.0 nM 7.85
CHEMBL4099048 — IC50 = 15.0 nM 7.82
CHEMBL221959 TOFACITINIB IC50 = 15.0 nM 7.82
CHEMBL4063642 — IC50 = 17.0 nM 7.77
CHEMBL4066404 — IC50 = 19.0 nM 7.72
CHEMBL4059894 — IC50 = 19.0 nM 7.72
CHEMBL4104105 — IC50 = 21.0 nM 7.68
CHEMBL3655080 — IC50 = 22.0 nM 7.66
CHEMBL3655104 — IC50 = 22.0 nM 7.66
CHEMBL3655086 — IC50 = 28.0 nM 7.55
CHEMBL3655081 ABROCITINIB IC50 = 29.0 nM 7.54
CHEMBL4093643 — IC50 = 30.0 nM 7.52
CHEMBL4059667 — IC50 = 31.0 nM 7.51
CHEMBL4085264 — IC50 = 36.0 nM 7.44
CHEMBL4087044 — IC50 = 37.0 nM 7.43
CHEMBL4089286 — IC50 = 39.0 nM 7.41
CHEMBL4090590 — IC50 = 40.0 nM 7.40
CHEMBL3655095 — IC50 = 42.0 nM 7.38
CHEMBL3655097 — IC50 = 51.0 nM 7.29
CHEMBL4075575 — IC50 = 52.0 nM 7.28
CHEMBL4100048 — IC50 = 57.0 nM 7.24
CHEMBL4098094 — IC50 = 70.0 nM 7.16
CHEMBL4065613 — IC50 = 85.0 nM 7.07
CHEMBL4100431 — IC50 = 90.0 nM 7.05
CHEMBL4085011 — IC50 = 92.0 nM 7.04
CHEMBL4078655 — IC50 = 123.0 nM 6.91
CHEMBL4071850 — IC50 = 141.0 nM 6.85
CHEMBL4082035 — IC50 = 144.0 nM 6.84
CHEMBL4092805 — IC50 = 178.0 nM 6.75
CHEMBL4101725 — IC50 = 572.0 nM 6.24