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Assay Detail

CHEMBL749392

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

Binding
Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells
6
Total Activities
5
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

Piperidine-ether based hNK1 antagonists 1: Determination of the relative and absolute stereochemical requirements
Harrison T, Williams B, Swain C, Ball R
Bioorg Med Chem Lett (1994) 4 : 2545 -2550
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.02 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16192 CP-96345 1 9.15
CHEMBL27006 1 9.00
CHEMBL85047 2 8.85
CHEMBL84588 1 8.15
CHEMBL315532 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16192 CP-96345 IC50 = 0.7 nM 9.15
CHEMBL27006 IC50 = 1.0 nM 9.00
CHEMBL85047 IC50 = 1.4 nM 8.85
CHEMBL84588 IC50 = 7.0 nM 8.15
CHEMBL315532 IC50 = 300.0 nM 6.52
CHEMBL85047 IC50 = 350.0 nM 6.46