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Assay Detail

CHEMBL747297

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

Binding
Binding affinity of compound was determined from inhibition of [125I]- substance P binding to the hNK1 receptor in CHO cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Acyclic NK1 antagonists: Replacements for the benzhydryl group.
Swain C, Cascieri M, Owens A, Saari W, Sadowski S, Strader C, Teall M, Van Niel M, Williams B
Bioorg Med Chem Lett (1994) 4 : 2161 -2164
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.50 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL417784 1 8.03
CHEMBL71498 1 7.26
CHEMBL433107 1 7.10
CHEMBL69051 1 7.03
CHEMBL305274 1 6.32
CHEMBL302719 1 5.94
CHEMBL68670 1 5.63
CHEMBL68934 1 5.63
CHEMBL71553 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL417784 IC50 = 9.3 nM 8.03
CHEMBL71498 IC50 = 55.0 nM 7.26
CHEMBL433107 IC50 = 80.0 nM 7.10
CHEMBL69051 IC50 = 93.0 nM 7.03
CHEMBL305274 IC50 = 483.0 nM 6.32
CHEMBL302719 IC50 = 1160.0 nM 5.94
CHEMBL68670 IC50 = 2333.0 nM 5.63
CHEMBL68934 IC50 = 2333.0 nM 5.63
CHEMBL71553 IC50 = 2500.0 nM 5.60