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Assay Detail

CHEMBL4713239

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Binding
Inhibition of recombinant JAK1 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay
ChEMBL ↗
54
Total Activities
53
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

Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors.
Park E,Lee SJ,Moon H,Park J,Jeon H,Hwang JS,Hwang H,Hong KB,Han SH,Choi S,Kang S
J Med Chem (2021) 64 : 958 -979
PubMed 33428419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 7.47 9.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4783938 — — 1 9.84
CHEMBL4761365 — — 2 9.70
CHEMBL4747742 — — 1 9.11
CHEMBL4789693 — — 1 8.95
CHEMBL221959 TOFACITINIB 4.0 1 8.81
CHEMBL4744772 — — 1 8.71
CHEMBL4779060 — — 1 8.50
CHEMBL4750779 — — 1 8.47
CHEMBL4777577 — — 1 8.25
CHEMBL4785998 — — 1 8.16
CHEMBL4742766 — — 1 8.11
CHEMBL4787133 — — 1 8.06
CHEMBL4759666 — — 1 8.03
CHEMBL4744048 — — 1 7.97
CHEMBL4781706 — — 1 7.92
CHEMBL4755612 — — 1 7.89
CHEMBL4785910 — — 1 7.82
CHEMBL4777200 — — 1 7.77
CHEMBL4787731 — — 1 7.76
CHEMBL4787974 — — 1 7.76
CHEMBL4763801 — — 1 7.75
CHEMBL4779340 — — 1 7.62
CHEMBL3301607 FILGOTINIB 4.0 1 7.58
CHEMBL4746186 — — 1 7.56
CHEMBL4741376 — — 1 7.52
CHEMBL4747285 — — 1 7.49
CHEMBL4786466 — — 1 7.47
CHEMBL4761631 — — 1 7.42
CHEMBL4759320 — — 1 7.39
CHEMBL4795901 — — 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4783938 — IC50 = 0.145 nM 9.84
CHEMBL4761365 — IC50 = 0.199 nM 9.70
CHEMBL4747742 — IC50 = 0.769 nM 9.11
CHEMBL4789693 — IC50 = 1.12 nM 8.95
CHEMBL221959 TOFACITINIB IC50 = 1.55 nM 8.81
CHEMBL4744772 — IC50 = 1.93 nM 8.71
CHEMBL4779060 — IC50 = 3.13 nM 8.50
CHEMBL4750779 — IC50 = 3.36 nM 8.47
CHEMBL4777577 — IC50 = 5.67 nM 8.25
CHEMBL4785998 — IC50 = 6.87 nM 8.16
CHEMBL4742766 — IC50 = 7.86 nM 8.11
CHEMBL4787133 — IC50 = 8.61 nM 8.06
CHEMBL4759666 — IC50 = 9.43 nM 8.03
CHEMBL4744048 — IC50 = 10.6 nM 7.97
CHEMBL4781706 — IC50 = 12.0 nM 7.92
CHEMBL4755612 — IC50 = 12.9 nM 7.89
CHEMBL4785910 — IC50 = 15.3 nM 7.82
CHEMBL4777200 — IC50 = 17.0 nM 7.77
CHEMBL4787731 — IC50 = 17.2 nM 7.76
CHEMBL4787974 — IC50 = 17.4 nM 7.76
CHEMBL4763801 — IC50 = 18.0 nM 7.75
CHEMBL4779340 — IC50 = 23.8 nM 7.62
CHEMBL3301607 FILGOTINIB IC50 = 26.2 nM 7.58
CHEMBL4746186 — IC50 = 27.6 nM 7.56
CHEMBL4741376 — IC50 = 30.5 nM 7.52
CHEMBL4747285 — IC50 = 32.7 nM 7.49
CHEMBL4786466 — IC50 = 33.8 nM 7.47
CHEMBL4761631 — IC50 = 37.7 nM 7.42
CHEMBL4759320 — IC50 = 40.8 nM 7.39
CHEMBL4795901 — IC50 = 46.1 nM 7.34
CHEMBL4750605 — IC50 = 60.0 nM 7.22
CHEMBL4747270 — IC50 = 65.0 nM 7.19
CHEMBL4761365 — IC50 = 70.7 nM 7.15
CHEMBL4746952 — IC50 = 72.2 nM 7.14
CHEMBL4796134 — IC50 = 74.9 nM 7.13
CHEMBL4742822 — IC50 = 80.1 nM 7.10
CHEMBL4781679 — IC50 = 82.0 nM 7.09
CHEMBL3593765 — IC50 = 88.0 nM 7.06
CHEMBL4749677 — IC50 = 93.4 nM 7.03
CHEMBL4750665 — IC50 = 114.0 nM 6.94
CHEMBL4781885 — IC50 = 132.0 nM 6.88
CHEMBL4743705 — IC50 = 149.0 nM 6.83
CHEMBL4764186 — IC50 = 160.0 nM 6.80
CHEMBL4757909 — IC50 = 195.0 nM 6.71
CHEMBL4763821 — IC50 = 202.0 nM 6.70
CHEMBL4754206 — IC50 = 215.0 nM 6.67
CHEMBL4784031 — IC50 = 243.0 nM 6.61
CHEMBL4777950 — IC50 = 400.0 nM 6.40
CHEMBL4756788 — IC50 = 406.0 nM 6.39
CHEMBL4791234 — IC50 = 827.0 nM 6.08