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Assay Detail

CHEMBL1840116

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Binding
Inhibition of JAK3
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK3 (CHEMBL2148)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Lim J, Taoka B, Otte RD, Spencer K, Dinsmore CJ, Altman MD, Chan G, Rosenstein C, Sharma S, Su HP, Szewczak AA, Xu L, Yin H, Zugay-Murphy J, Marshall CG, Young JR.
J Med Chem (2011) 54 : 7334 -7349
PubMed 21942426 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.14 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261386 1 7.11
CHEMBL1834949 1 6.14
CHEMBL1835014 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261386 IC50 = 77.0 nM 7.11
CHEMBL1834949 IC50 = 720.0 nM 6.14
CHEMBL1835014 IC50 = 6800.0 nM 5.17