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Assay Detail

CHEMBL745034

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

Binding
Tested for binding affinity by measuring displacement of [125I]SP from human NK-1 receptor in CHO Cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Quinuclidine based NK-1 antagonists 2: determination of the absolute stereochemical requirements
Swain C, Seward E, Sabin V, Owen S, Baker R, Cascieri M, Sadowski S, Strader C, Ball R
Bioorg Med Chem Lett (1993) 3 : 1703 -1706
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.71 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49638 1 9.15
CHEMBL22194 L-709210 1 8.89
CHEMBL296228 1 6.57
CHEMBL297068 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49638 IC50 = 0.7 nM 9.15
CHEMBL22194 L-709210 IC50 = 1.3 nM 8.89
CHEMBL296228 IC50 = 270.0 nM 6.57
CHEMBL297068 IC50 = 570.0 nM 6.24