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Assay Detail

CHEMBL828104

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

Binding
Inhibition of substance P binding to Tachykinin receptor 1 in Chinese hamster ovary cells
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type ovary
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Successful virtual screening for a submicromolar antagonist of the neurokinin-1 receptor based on a ligand-supported homology model.
Evers A, Klebe G.
J Med Chem (2004) 47 : 5381 -5392
PubMed 15481976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.41 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99055 1 10.30
CHEMBL356062 1 10.22
CHEMBL107482 1 9.68
CHEMBL28055 2 9.28
CHEMBL441225 CP-99994 1 9.22
CHEMBL422931 1 9.00
CHEMBL22194 L-709210 1 8.89
CHEMBL188166 1 8.80
CHEMBL417784 1 8.03
CHEMBL281940 1 7.97
CHEMBL427514 1 7.92
CHEMBL187554 1 7.17
CHEMBL361031 1 6.60
CHEMBL56176 1 6.40
CHEMBL360815 1 5.81
CHEMBL188529 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99055 IC50 = 0.05 nM 10.30
CHEMBL356062 IC50 = 0.06 nM 10.22
CHEMBL107482 IC50 = 0.21 nM 9.68
CHEMBL28055 IC50 = 0.53 nM 9.28
CHEMBL28055 IC50 = 0.53 nM 9.28
CHEMBL441225 CP-99994 IC50 = 0.6 nM 9.22
CHEMBL422931 IC50 = 1.0 nM 9.00
CHEMBL22194 L-709210 IC50 = 1.3 nM 8.89
CHEMBL188166 IC50 = 1.6 nM 8.80
CHEMBL417784 IC50 = 9.3 nM 8.03
CHEMBL281940 IC50 = 10.7 nM 7.97
CHEMBL427514 IC50 = 12.0 nM 7.92
CHEMBL187554 IC50 = 67.0 nM 7.17
CHEMBL361031 IC50 = 250.0 nM 6.60
CHEMBL56176 IC50 = 400.0 nM 6.40
CHEMBL360815 IC50 = 1533.0 nM 5.81
CHEMBL188529 IC50 > 10000.0 nM -