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Assay Detail

CHEMBL1828296

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Binding
Inhibition of KIT activity by TR-FRET assay
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

Mast/stem cell growth factor receptor Kit (CHEMBL1936)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Kinoshita K, Kobayashi T, Asoh K, Furuichi N, Ito T, Kawada H, Hara S, Ohwada J, Hattori K, Miyagi T, Hong WS, Park MJ, Takanashi K, Tsukaguchi T, Sakamoto H, Tsukuda T, Oikawa N.
J Med Chem (2011) 54 : 6286 -6294
PubMed 21823617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.67 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823219 1 7.30
CHEMBL1779201 1 7.08
CHEMBL1823220 1 5.62
CHEMBL1823361 1 -
CHEMBL1823223 1 -
CHEMBL1823222 1 -
CHEMBL1823221 1 -
CHEMBL1779202 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823219 IC50 = 49.8 nM 7.30
CHEMBL1779201 IC50 = 83.9 nM 7.08
CHEMBL1823220 IC50 = 2422.0 nM 5.62
CHEMBL1823361 IC50 > 5000.0 nM -
CHEMBL1823223 IC50 > 5000.0 nM -
CHEMBL1823222 IC50 > 5000.0 nM -
CHEMBL1823221 IC50 > 5000.0 nM -
CHEMBL1779202 IC50 > 50000.0 nM -