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Assay Detail

CHEMBL751900

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

Binding
Inhibition of [125I]-Substance P binding to human NK1 receptors in CHO cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists.
Mills SG, Wu MT, MacCoss M, Budhu RJ, Dorn CP, Cascieri MA, Sadowski S, Strader CD, Greenlee WJ
Bioorg Med Chem Lett (1993) 3 : 2707 -2712
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.99 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16192 CP-96345 1 9.30
CHEMBL93401 1 8.05
CHEMBL91438 1 8.05
CHEMBL92621 1 7.96
CHEMBL431459 1 7.77
CHEMBL90416 1 7.39
CHEMBL90547 1 7.26
CHEMBL314084 1 7.24
CHEMBL63109 1 6.89
CHEMBL329416 1 6.85
CHEMBL93038 1 6.70
CHEMBL441458 1 6.66
CHEMBL93251 1 6.57
CHEMBL299887 1 6.55
CHEMBL329168 1 6.54
CHEMBL59854 1 6.30
CHEMBL90035 1 6.22
CHEMBL329840 1 6.03
CHEMBL329445 1 5.97
CHEMBL59913 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16192 CP-96345 IC50 = 0.5 nM 9.30
CHEMBL93401 IC50 = 9.0 nM 8.05
CHEMBL91438 IC50 = 9.0 nM 8.05
CHEMBL92621 IC50 = 11.0 nM 7.96
CHEMBL431459 IC50 = 17.0 nM 7.77
CHEMBL90416 IC50 = 41.0 nM 7.39
CHEMBL90547 IC50 = 55.0 nM 7.26
CHEMBL314084 IC50 = 57.0 nM 7.24
CHEMBL63109 IC50 = 130.0 nM 6.89
CHEMBL329416 IC50 = 140.0 nM 6.85
CHEMBL93038 IC50 = 200.0 nM 6.70
CHEMBL441458 IC50 = 217.0 nM 6.66
CHEMBL93251 IC50 = 267.0 nM 6.57
CHEMBL299887 IC50 = 280.0 nM 6.55
CHEMBL329168 IC50 = 290.0 nM 6.54
CHEMBL59854 IC50 = 500.0 nM 6.30
CHEMBL90035 IC50 = 597.0 nM 6.22
CHEMBL329840 IC50 = 930.0 nM 6.03
CHEMBL329445 IC50 = 1080.0 nM 5.97
CHEMBL59913 IC50 = 3000.0 nM 5.52