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Assay Detail

CHEMBL4416473

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

Binding
Inhibition of recombinant human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in Sf1 cells using PolyGT-Biotin as substrate measured after 3 to 20 hrs by HTRF assay
35
Total Activities
35
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 JAK3 (CHEMBL2148)
Type SINGLE PROTEIN
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 35 7.96 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4526485 1 9.15
CHEMBL4471599 1 9.00
CHEMBL4482927 1 8.96
CHEMBL4526498 1 8.96
CHEMBL4443416 1 8.85
CHEMBL4460058 1 8.85
CHEMBL3393066 VS-5584 1.0 1 8.77
CHEMBL4536419 1 8.62
CHEMBL4448906 1 8.59
CHEMBL4450301 1 8.57
CHEMBL4558494 1 8.55
CHEMBL4536396 1 8.52
CHEMBL4556988 1 8.47
CHEMBL4463007 1 8.46
CHEMBL4550310 1 8.44
CHEMBL4469844 1 8.41
CHEMBL4574559 1 8.31
CHEMBL4517586 1 8.22
CHEMBL4467200 1 8.08
CHEMBL4520559 1 7.80
CHEMBL4587709 1 7.75
CHEMBL4476445 1 7.47
CHEMBL4463215 1 7.41
CHEMBL4458055 1 7.40
CHEMBL4438810 1 7.33
CHEMBL4568482 1 7.31
CHEMBL4476802 1 7.28
CHEMBL4467503 1 7.23
CHEMBL4549136 1 7.19
CHEMBL4446722 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4526485 IC50 = 0.7 nM 9.15
CHEMBL4471599 IC50 = 1.0 nM 9.00
CHEMBL4482927 IC50 = 1.1 nM 8.96
CHEMBL4526498 IC50 = 1.1 nM 8.96
CHEMBL4443416 IC50 = 1.4 nM 8.85
CHEMBL4460058 IC50 = 1.4 nM 8.85
CHEMBL3393066 VS-5584 IC50 = 1.7 nM 8.77
CHEMBL4536419 IC50 = 2.4 nM 8.62
CHEMBL4448906 IC50 = 2.6 nM 8.59
CHEMBL4450301 IC50 = 2.7 nM 8.57
CHEMBL4558494 IC50 = 2.8 nM 8.55
CHEMBL4536396 IC50 = 3.0 nM 8.52
CHEMBL4556988 IC50 = 3.4 nM 8.47
CHEMBL4463007 IC50 = 3.5 nM 8.46
CHEMBL4550310 IC50 = 3.6 nM 8.44
CHEMBL4469844 IC50 = 3.9 nM 8.41
CHEMBL4574559 IC50 = 4.9 nM 8.31
CHEMBL4517586 IC50 = 6.0 nM 8.22
CHEMBL4467200 IC50 = 8.4 nM 8.08
CHEMBL4520559 IC50 = 16.0 nM 7.80
CHEMBL4587709 IC50 = 18.0 nM 7.75
CHEMBL4476445 IC50 = 34.0 nM 7.47
CHEMBL4463215 IC50 = 39.0 nM 7.41
CHEMBL4458055 IC50 = 40.0 nM 7.40
CHEMBL4438810 IC50 = 47.0 nM 7.33
CHEMBL4568482 IC50 = 49.0 nM 7.31
CHEMBL4476802 IC50 = 53.0 nM 7.28
CHEMBL4467503 IC50 = 59.0 nM 7.23
CHEMBL4549136 IC50 = 64.0 nM 7.19
CHEMBL4446722 IC50 = 80.0 nM 7.10
CHEMBL4536380 IC50 = 80.0 nM 7.10
CHEMBL4441275 IC50 = 96.0 nM 7.02
CHEMBL4440240 IC50 = 260.0 nM 6.58
CHEMBL4571980 IC50 = 420.0 nM 6.38
CHEMBL4441500 IC50 = 490.0 nM 6.31