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Assay Detail

CHEMBL4347596

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

Binding
Inhibition of recombinant human JAK2 using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 60 mins by LANCE assay
27
Total Activities
27
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 JAK2 (CHEMBL2971)
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 27 7.76 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4453646 1 8.70
CHEMBL4526274 1 8.40
CHEMBL4564021 1 8.30
CHEMBL4466059 1 8.30
CHEMBL4462229 1 8.15
CHEMBL4549369 1 8.00
CHEMBL4457617 1 8.00
CHEMBL4471710 1 8.00
CHEMBL4443462 1 7.92
CHEMBL4575813 1 7.85
CHEMBL4520721 1 7.82
CHEMBL4559926 1 7.75
CHEMBL4556463 1 7.70
CHEMBL4563723 1 7.68
CHEMBL4592912 1 7.66
CHEMBL4469297 1 7.52
CHEMBL4451298 1 7.44
CHEMBL4575735 1 7.44
CHEMBL4540416 1 7.37
CHEMBL4533614 1 7.34
CHEMBL4568644 1 7.34
CHEMBL4562491 1 7.30
CHEMBL4584008 1 7.21
CHEMBL4439450 1 7.07
CHEMBL4441124 1 -
CHEMBL4538220 1 -
CHEMBL4581017 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4453646 IC50 = 2.0 nM 8.70
CHEMBL4526274 IC50 = 4.0 nM 8.40
CHEMBL4564021 IC50 = 5.0 nM 8.30
CHEMBL4466059 IC50 = 5.0 nM 8.30
CHEMBL4462229 IC50 = 7.0 nM 8.15
CHEMBL4549369 IC50 = 10.0 nM 8.00
CHEMBL4457617 IC50 = 10.0 nM 8.00
CHEMBL4471710 IC50 = 10.0 nM 8.00
CHEMBL4443462 IC50 = 12.0 nM 7.92
CHEMBL4575813 IC50 = 14.0 nM 7.85
CHEMBL4520721 IC50 = 15.0 nM 7.82
CHEMBL4559926 IC50 = 18.0 nM 7.75
CHEMBL4556463 IC50 = 20.0 nM 7.70
CHEMBL4563723 IC50 = 21.0 nM 7.68
CHEMBL4592912 IC50 = 22.0 nM 7.66
CHEMBL4469297 IC50 = 30.0 nM 7.52
CHEMBL4451298 IC50 = 36.0 nM 7.44
CHEMBL4575735 IC50 = 36.0 nM 7.44
CHEMBL4540416 IC50 = 43.0 nM 7.37
CHEMBL4533614 IC50 = 46.0 nM 7.34
CHEMBL4568644 IC50 = 46.0 nM 7.34
CHEMBL4562491 IC50 = 50.0 nM 7.30
CHEMBL4584008 IC50 = 61.0 nM 7.21
CHEMBL4439450 IC50 = 85.0 nM 7.07
CHEMBL4441124 IC50 > 100.0 nM -
CHEMBL4538220 IC50 > 100.0 nM -
CHEMBL4581017 IC50 > 100.0 nM -