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Assay Detail

CHEMBL4347601

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

Binding
Inhibition of recombinant human JAK1 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay
6
Total Activities
6
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 of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies.
Liang X, Zang J, Li X, Tang S, Huang M, Geng M, Chou CJ, Li C, Cao Y, Xu W, Liu H, Zhang Y.
J Med Chem (2019) 62 : 3898 -3923
PubMed 30901208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.00 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4453646 1 8.47
CHEMBL4526274 1 8.32
CHEMBL4575813 1 8.00
CHEMBL4466059 1 7.85
CHEMBL4471710 1 7.82
CHEMBL4562491 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4453646 IC50 = 3.4 nM 8.47
CHEMBL4526274 IC50 = 4.8 nM 8.32
CHEMBL4575813 IC50 = 10.0 nM 8.00
CHEMBL4466059 IC50 = 14.0 nM 7.85
CHEMBL4471710 IC50 = 15.0 nM 7.82
CHEMBL4562491 IC50 = 30.0 nM 7.52