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Assay Detail

CHEMBL4236469

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ADMET
Inhibition of recombinant human N-terminal His-tagged JAK2 catalytic domain (826 to 1132 residues) expressed in baculovirus expression system using Biotin-Lyn-Substrate2 after 1 hr by ELISA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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 and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor.
Hamaguchi H, Amano Y, Moritomo A, Shirakami S, Nakajima Y, Nakai K, Nomura N, Ito M, Higashi Y, Inoue T.
Bioorg Med Chem (2018) 26 : 4971 -4983
PubMed 30145050 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.00 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4238926 1 8.77
CHEMBL4246788 1 8.30
CHEMBL4242999 1 8.30
CHEMBL4247874 1 7.96
CHEMBL4249444 1 7.96
CHEMBL4241916 1 7.82
CHEMBL4239361 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4238926 IC50 = 1.7 nM 8.77
CHEMBL4246788 IC50 = 5.0 nM 8.30
CHEMBL4242999 IC50 = 5.0 nM 8.30
CHEMBL4247874 IC50 = 11.0 nM 7.96
CHEMBL4249444 IC50 = 11.0 nM 7.96
CHEMBL4241916 IC50 = 15.0 nM 7.82
CHEMBL4239361 IC50 = 120.0 nM 6.92