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Assay Detail

CHEMBL1657304

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

Binding
Inhibition of GST-tagged Jak3 expressed in insect cells using 18 uM ATP
8
Total Activities
8
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

Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.
Thoma G, Nuninger F, Falchetto R, Hermes E, Tavares GA, Vangrevelinghe E, Zerwes HG.
J Med Chem (2011) 54 : 284 -288
PubMed 21155605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.26 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1650951 1 8.10
CHEMBL221959 TOFACITINIB 4.0 1 8.10
CHEMBL1235315 1 7.57
CHEMBL1650955 1 7.44
CHEMBL1650953 1 6.88
CHEMBL1650954 1 6.37
CHEMBL1650956 1 6.34
CHEMBL1650952 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1650951 IC50 = 8.0 nM 8.10
CHEMBL221959 TOFACITINIB IC50 = 8.0 nM 8.10
CHEMBL1235315 IC50 = 27.0 nM 7.57
CHEMBL1650955 IC50 = 36.0 nM 7.44
CHEMBL1650953 IC50 = 133.0 nM 6.88
CHEMBL1650954 IC50 = 423.0 nM 6.37
CHEMBL1650956 IC50 = 460.0 nM 6.34
CHEMBL1650952 IC50 > 10000.0 nM -