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Assay Detail

CHEMBL750291

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

Functional
Antagonism of NK1 receptor in rat liver microsomes.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Expert

Target

Substance-P receptor (CHEMBL4027)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3-Benzyloxy-2-phenylpiperidine NK1 antagonists: the influence of alpha methyl substitution
Swain C, Williams B, Baker R, Cascieri M, Chicchi G, Forrest M, Herbert R, Keown L, Ladduwahetty T, Luell S, MacIntyre D, Metzger J, Morton S, Owens A, Sadowski S, Watt A
Bioorg Med Chem Lett (1997) 7 : 2959 -2962
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.55 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL100636 1 10.05
CHEMBL102032 1 9.82
CHEMBL101148 1 9.80
CHEMBL98524 1 9.80
CHEMBL99792 1 9.74
CHEMBL27006 1 9.10
CHEMBL102157 1 9.04
CHEMBL317979 1 8.23
CHEMBL418800 1 7.60
CHEMBL319212 1 7.07
CHEMBL103657 1 7.07
CHEMBL316486 1 7.06
CHEMBL100178 1 6.80
CHEMBL2111607 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL100636 IC50 = 0.09 nM 10.05
CHEMBL102032 IC50 = 0.15 nM 9.82
CHEMBL101148 IC50 = 0.16 nM 9.80
CHEMBL98524 IC50 = 0.16 nM 9.80
CHEMBL99792 IC50 = 0.18 nM 9.74
CHEMBL27006 IC50 = 0.8 nM 9.10
CHEMBL102157 IC50 = 0.91 nM 9.04
CHEMBL317979 IC50 = 5.9 nM 8.23
CHEMBL418800 IC50 = 25.0 nM 7.60
CHEMBL319212 IC50 = 85.0 nM 7.07
CHEMBL103657 IC50 = 86.0 nM 7.07
CHEMBL316486 IC50 = 87.0 nM 7.06
CHEMBL100178 IC50 = 160.0 nM 6.80
CHEMBL2111607 IC50 > 10000.0 nM -