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Assay Detail

CHEMBL2160981

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

Binding
Displacement of [3H]astemizole from human ERG potassium channel
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).
Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE.
J Med Chem (2011) 54 : 7860 -7883
PubMed 22039836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.11 5.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2158224 1 5.11
CHEMBL2158290 1 -
CHEMBL2158222 1 -
CHEMBL2158223 1 -
CHEMBL2158225 1 -
CHEMBL2158226 1 -
CHEMBL2158227 1 -
CHEMBL2158228 1 -
CHEMBL2158229 1 -
CHEMBL2158230 1 -
CHEMBL256712 1 -
CHEMBL2158231 1 -
CHEMBL1908842 1 -
CHEMBL2158287 1 -
CHEMBL2158288 1 -
CHEMBL2158221 1 -
CHEMBL2158291 1 -
CHEMBL2158292 1 -
CHEMBL2158293 1 -
CHEMBL2158294 1 -
CHEMBL2158295 1 -
CHEMBL2158296 1 -
CHEMBL2158297 1 -
CHEMBL2158298 1 -
CHEMBL2158299 1 -
CHEMBL2158300 1 -
CHEMBL2158301 1 -
CHEMBL2158302 1 -
CHEMBL2158303 1 -
CHEMBL2158289 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2158224 IC50 = 7700.0 nM 5.11
CHEMBL2158290 IC50 > 10000.0 nM -
CHEMBL2158222 IC50 - -
CHEMBL2158223 IC50 - -
CHEMBL2158225 IC50 > 10000.0 nM -
CHEMBL2158226 IC50 - -
CHEMBL2158227 IC50 > 10000.0 nM -
CHEMBL2158228 IC50 - -
CHEMBL2158229 IC50 - -
CHEMBL2158230 IC50 > 10000.0 nM -
CHEMBL256712 IC50 > 3200.0 nM -
CHEMBL2158231 IC50 > 10000.0 nM -
CHEMBL1908842 IC50 > 10000.0 nM -
CHEMBL2158287 IC50 - -
CHEMBL2158288 IC50 - -
CHEMBL2158221 IC50 > 10000.0 nM -
CHEMBL2158291 IC50 - -
CHEMBL2158292 IC50 - -
CHEMBL2158293 IC50 - -
CHEMBL2158294 IC50 > 10000.0 nM -
CHEMBL2158295 IC50 - -
CHEMBL2158296 IC50 > 10000.0 nM -
CHEMBL2158297 IC50 > 3200.0 nM -
CHEMBL2158298 IC50 - -
CHEMBL2158299 IC50 > 10000.0 nM -
CHEMBL2158300 IC50 - -
CHEMBL2158301 IC50 > 10000.0 nM -
CHEMBL2158302 IC50 > 10000.0 nM -
CHEMBL2158303 IC50 - -
CHEMBL2158289 IC50 > 10000.0 nM -