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Assay Detail

CHEMBL745035

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Functional
Neurokinin (NK1) receptor antagonistic activity was evaluated.
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Substance-P receptor (CHEMBL3942)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and NK1 receptor antagonistic activity of (+/-)-1-acyl-3-(3,4- dichlorophenyl)-3-[2-(spiro-substituted piperidin-1'-yl)ethyl]piperidines.
Kubota H, Okamoto Y, Fujii M, Ikeda K, Takeuchi M, Shibanuma T, Isomura Y.
Bioorg Med Chem Lett (1998) 8 : 1541 -1546
PubMed 9873386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.01 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38763 1 10.72
CHEMBL288600 1 9.51
CHEMBL288123 2 8.72
CHEMBL289727 1 8.70
CHEMBL39595 1 8.32
CHEMBL38030 1 8.20
CHEMBL1201933 1 7.80
CHEMBL288840 1 7.80
CHEMBL38624 1 7.75
CHEMBL38652 1 7.51
CHEMBL262540 1 7.27
CHEMBL39232 1 7.24
CHEMBL1794935 1 6.98
CHEMBL39049 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38763 IC50 = 0.019 nM 10.72
CHEMBL288600 IC50 = 0.31 nM 9.51
CHEMBL288123 IC50 = 1.9 nM 8.72
CHEMBL289727 IC50 = 2.0 nM 8.70
CHEMBL39595 IC50 = 4.8 nM 8.32
CHEMBL38030 IC50 = 6.3 nM 8.20
CHEMBL1201933 IC50 = 16.0 nM 7.80
CHEMBL288840 IC50 = 16.0 nM 7.80
CHEMBL38624 IC50 = 18.0 nM 7.75
CHEMBL38652 IC50 = 31.0 nM 7.51
CHEMBL288123 IC50 = 35.0 nM 7.46
CHEMBL262540 IC50 = 54.0 nM 7.27
CHEMBL39232 IC50 = 58.0 nM 7.24
CHEMBL1794935 IC50 = 105.0 nM 6.98
CHEMBL39049 IC50 = 710.0 nM 6.15