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Assay Detail

CHEMBL4416477

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

Binding
Inhibition of JAK1/3 in human Ramos cells harboring beta-lactamase reporter gene assessed as reduction in IL4-induced STAT6 phosphorylation incubated for 2 hrs by FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

JAK3/JAK1 (CHEMBL3038491)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.
Bach J, Eastwood P, González J, Gómez E, Alonso JA, Fonquerna S, Lozoya E, Orellana A, Maldonado M, Calaf E, Albertí J, Pérez J, Andrés A, Prats N, Carreño C, Calama E, De Alba J, Calbet M, Miralpeix M, Ramis I.
J Med Chem (2019) 62 : 9045 -9060
PubMed 31609613 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.69 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463007 1 7.39
CHEMBL4482927 1 7.36
CHEMBL4526485 1 7.34
CHEMBL4460058 1 7.17
CHEMBL4526498 1 7.12
CHEMBL4558494 1 7.02
CHEMBL4536419 1 6.89
CHEMBL4556988 1 6.89
CHEMBL4517586 1 6.89
CHEMBL4458055 1 6.85
CHEMBL4463215 1 6.46
CHEMBL4550310 1 6.12
CHEMBL4476445 1 5.96
CHEMBL4443416 1 5.47
CHEMBL4587709 1 5.47
CHEMBL4520559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463007 IC50 = 41.0 nM 7.39
CHEMBL4482927 IC50 = 44.0 nM 7.36
CHEMBL4526485 IC50 = 46.0 nM 7.34
CHEMBL4460058 IC50 = 68.0 nM 7.17
CHEMBL4526498 IC50 = 76.0 nM 7.12
CHEMBL4558494 IC50 = 96.0 nM 7.02
CHEMBL4536419 IC50 = 130.0 nM 6.89
CHEMBL4556988 IC50 = 130.0 nM 6.89
CHEMBL4517586 IC50 = 130.0 nM 6.89
CHEMBL4458055 IC50 = 140.0 nM 6.85
CHEMBL4463215 IC50 = 350.0 nM 6.46
CHEMBL4550310 IC50 = 760.0 nM 6.12
CHEMBL4476445 IC50 = 1100.0 nM 5.96
CHEMBL4443416 IC50 = 3400.0 nM 5.47
CHEMBL4587709 IC50 = 3400.0 nM 5.47
CHEMBL4520559 IC50 - -