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Assay Detail

CHEMBL5377862

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

Binding
Inhibition of recombinant JAK1 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr by TR-FRET Lanthascreen assay
40
Total Activities
37
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 and Biological Evaluation of a Potent and Selective JAK1 Inhibitor for the Treatment of Pulmonary Fibrosis.
Park E, Park S, Lee SJ, Jeong D, Jin H, Moon H, Cha B, Kim D, Ma S, Seo W, Han SH, Lee YS, Kang S.
J Med Chem (2023) 66 : 16342 -16363
PubMed 38031930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 8.09 10.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5397297 1 10.36
CHEMBL5398372 2 9.25
CHEMBL5413283 1 9.24
CHEMBL5423944 1 9.20
CHEMBL5405043 2 9.10
CHEMBL5408324 2 8.96
CHEMBL221959 TOFACITINIB 4.0 1 8.90
CHEMBL5410919 1 8.73
CHEMBL5393770 1 8.63
CHEMBL5441087 1 8.61
CHEMBL5427932 1 8.59
CHEMBL5405140 1 8.57
CHEMBL5435417 1 8.54
CHEMBL5440017 1 8.53
CHEMBL5439582 1 8.48
CHEMBL5434116 1 8.30
CHEMBL5430795 1 8.28
CHEMBL5404261 1 8.25
CHEMBL5423387 1 8.19
CHEMBL5410927 1 8.04
CHEMBL5413771 1 8.03
CHEMBL5423894 1 7.99
CHEMBL5420407 1 7.95
CHEMBL5400756 1 7.93
CHEMBL4742766 1 7.89
CHEMBL3301607 FILGOTINIB 4.0 1 7.78
CHEMBL5396523 1 7.78
CHEMBL5396079 1 7.56
CHEMBL5417546 1 7.47
CHEMBL5430831 1 7.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5397297 IC50 = 0.044 nM 10.36
CHEMBL5398372 IC50 = 0.563 nM 9.25
CHEMBL5413283 IC50 = 0.577 nM 9.24
CHEMBL5423944 IC50 = 0.637 nM 9.20
CHEMBL5405043 IC50 = 0.799 nM 9.10
CHEMBL5408324 IC50 = 1.1 nM 8.96
CHEMBL221959 TOFACITINIB IC50 = 1.26 nM 8.90
CHEMBL5410919 IC50 = 1.86 nM 8.73
CHEMBL5393770 IC50 = 2.34 nM 8.63
CHEMBL5441087 IC50 = 2.46 nM 8.61
CHEMBL5427932 IC50 = 2.59 nM 8.59
CHEMBL5405140 IC50 = 2.691 nM 8.57
CHEMBL5435417 IC50 = 2.86 nM 8.54
CHEMBL5440017 IC50 = 2.934 nM 8.53
CHEMBL5439582 IC50 = 3.32 nM 8.48
CHEMBL5434116 IC50 = 5.0 nM 8.30
CHEMBL5430795 IC50 = 5.26 nM 8.28
CHEMBL5404261 IC50 = 5.68 nM 8.25
CHEMBL5423387 IC50 = 6.51 nM 8.19
CHEMBL5410927 IC50 = 9.23 nM 8.04
CHEMBL5413771 IC50 = 9.38 nM 8.03
CHEMBL5423894 IC50 = 10.2 nM 7.99
CHEMBL5420407 IC50 = 11.3 nM 7.95
CHEMBL5400756 IC50 = 11.7 nM 7.93
CHEMBL4742766 IC50 = 12.9 nM 7.89
CHEMBL3301607 FILGOTINIB IC50 = 16.5 nM 7.78
CHEMBL5396523 IC50 = 16.6 nM 7.78
CHEMBL5396079 IC50 = 27.6 nM 7.56
CHEMBL5417546 IC50 = 34.2 nM 7.47
CHEMBL5430831 IC50 = 35.6 nM 7.45
CHEMBL5440026 IC50 = 37.9 nM 7.42
CHEMBL5440077 IC50 = 49.4 nM 7.31
CHEMBL5405043 IC50 = 56.1 nM 7.25
CHEMBL5408389 IC50 = 57.6 nM 7.24
CHEMBL5408324 IC50 = 76.8 nM 7.12
CHEMBL5440699 IC50 = 82.2 nM 7.08
CHEMBL5397572 IC50 = 92.0 nM 7.04
CHEMBL5402123 IC50 = 97.5 nM 7.01
CHEMBL5398372 IC50 = 112.4 nM 6.95
CHEMBL5435251 IC50 = 285.6 nM 6.54