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Assay Detail

CHEMBL4124194

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ADMET
Inhibition of kinase tracer-05 binding to C-terminal NanoLuc tagged full length JAK2 (unknown origin) expressed in HEK cells by NanoBRET assay
4
Total Activities
4
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

Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.
Forster M, Chaikuad A, Dimitrov T, Döring E, Holstein J, Berger BT, Gehringer M, Ghoreschi K, Müller S, Knapp S, Laufer SA.
J Med Chem (2018) 61 : 5350 -5366
PubMed 29852068 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.66 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4125719 1 6.20
CHEMBL4128266 1 5.11
CHEMBL4128181 1 -
CHEMBL4125861 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4125719 EC50 = 630.0 nM 6.20
CHEMBL4128266 EC50 = 7710.0 nM 5.11
CHEMBL4128181 EC50 > 10000.0 nM -
CHEMBL4125861 EC50 > 10000.0 nM -