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Assay Detail

CHEMBL4414830

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

ADMET
Inhibition of cKIT (unknown origin)
9
Total Activities
9
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

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

Publication

Identification of <i>N</i>-Methyl Nicotinamide and <i>N</i>-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).
Moslin R, Zhang Y, Wrobleski ST, Lin S, Mertzman M, Spergel S, Tokarski JS, Strnad J, Gillooly K, McIntyre KW, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Heimrich E, Yang X, Muckelbauer JK, Chang C, Tredup J, Mulligan D, Xie D, Aranibar N, Chiney M, Burke JR, Lombardo L, Carter PH, Weinstein DS.
J Med Chem (2019) 62 : 8953 -8972
PubMed 31314518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.43 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4526283 1 7.00
CHEMBL4544320 1 6.20
CHEMBL4444606 1 6.08
CHEMBL4548200 1 -
CHEMBL4472802 1 -
CHEMBL4453545 1 -
CHEMBL4438202 1 -
CHEMBL4542289 1 -
CHEMBL4531793 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4526283 IC50 = 100.0 nM 7.00
CHEMBL4544320 IC50 = 630.0 nM 6.20
CHEMBL4444606 IC50 = 830.0 nM 6.08
CHEMBL4548200 IC50 > 2000.0 nM -
CHEMBL4472802 IC50 > 2000.0 nM -
CHEMBL4453545 IC50 > 2000.0 nM -
CHEMBL4438202 IC50 > 2000.0 nM -
CHEMBL4542289 IC50 > 2000.0 nM -
CHEMBL4531793 IC50 > 2000.0 nM -