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Assay Detail

CHEMBL871229

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

Binding
Displacement of [125I] labeled substance P from human cloned NK1 receptor expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

NK1 antagonists based on seven membered lactam scaffolds.
Elliott JM, Carlson EJ, Chicchi GG, Dirat O, Dominguez M, Gerhard U, Jelley R, Jones AB, Kurtz MM, Tsao Kl, Wheeldon A.
Bioorg Med Chem Lett (2006) 16 : 2929 -2932
PubMed 16574413 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 9.56 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL425956 1 10.05
CHEMBL437878 1 9.92
CHEMBL380680 1 9.85
CHEMBL210365 1 9.72
CHEMBL209657 1 9.66
CHEMBL209456 1 9.64
CHEMBL210630 1 9.55
CHEMBL209240 1 9.48
CHEMBL209407 1 9.39
CHEMBL380388 1 9.37
CHEMBL378663 1 9.36
CHEMBL413279 1 9.31
CHEMBL382255 1 9.28
CHEMBL379816 1 9.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL425956 IC50 = 0.09 nM 10.05
CHEMBL437878 IC50 = 0.12 nM 9.92
CHEMBL380680 IC50 = 0.14 nM 9.85
CHEMBL210365 IC50 = 0.19 nM 9.72
CHEMBL209657 IC50 = 0.22 nM 9.66
CHEMBL209456 IC50 = 0.23 nM 9.64
CHEMBL210630 IC50 = 0.28 nM 9.55
CHEMBL209240 IC50 = 0.33 nM 9.48
CHEMBL209407 IC50 = 0.41 nM 9.39
CHEMBL380388 IC50 = 0.43 nM 9.37
CHEMBL378663 IC50 = 0.44 nM 9.36
CHEMBL413279 IC50 = 0.49 nM 9.31
CHEMBL382255 IC50 = 0.53 nM 9.28
CHEMBL379816 IC50 = 0.64 nM 9.19