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Assay Detail

CHEMBL807900

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

Functional
Antagonist activity for Tachykinin receptor 1 as displacement of [3H]-Substance P in human IM-9 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type IM-9
Confidence 9 — Direct single protein target
Curated By Expert

Target

Substance-P receptor (CHEMBL249)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist.
Rosen TJ, Coffman KJ, McLean S, Crawford RT, Bryce DK, Gohda Y, Tsuchiya M, Nagahisa A, Nakane M, Lowe JA.
Bioorg Med Chem Lett (1998) 8 : 281 -284
PubMed 9871670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.44 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94461 1 10.05
CHEMBL329007 1 9.96
CHEMBL94328 1 9.85
CHEMBL437075 1 9.85
CHEMBL319301 1 9.74
CHEMBL319118 1 9.72
CHEMBL95852 1 9.39
CHEMBL95315 1 9.34
CHEMBL441225 CP-99994 1 9.31
CHEMBL98125 1 9.25
CHEMBL235363 SUBSTANCE P 1.0 1 9.21
CHEMBL320220 1 9.10
CHEMBL327357 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94461 IC50 = 0.09 nM 10.05
CHEMBL329007 IC50 = 0.11 nM 9.96
CHEMBL94328 IC50 = 0.14 nM 9.85
CHEMBL437075 IC50 = 0.14 nM 9.85
CHEMBL319301 IC50 = 0.18 nM 9.74
CHEMBL319118 IC50 = 0.19 nM 9.72
CHEMBL95852 IC50 = 0.41 nM 9.39
CHEMBL95315 IC50 = 0.46 nM 9.34
CHEMBL441225 CP-99994 IC50 = 0.49 nM 9.31
CHEMBL98125 IC50 = 0.56 nM 9.25
CHEMBL235363 SUBSTANCE P IC50 = 0.61 nM 9.21
CHEMBL320220 IC50 = 0.8 nM 9.10
CHEMBL327357 IC50 = 10.87 nM 7.96