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Assay Detail

CHEMBL880145

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

Binding
Binding affinity towards human mutant NK-1 receptor in which His-197 has been replaced by alanine (H197A)
6
Total Activities
6
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 NK1 antagonists, the role of the benzhydryl
Swain C, Fong T, Haworth K, Owen S, Seward E, Strader C
Bioorg Med Chem Lett (1995) 5 : 1261 -1264
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.15 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283356 L-706125 1 6.71
CHEMBL22194 L-709210 1 6.48
CHEMBL282657 1 6.30
CHEMBL435564 1 6.21
CHEMBL283979 1 6.07
CHEMBL277260 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283356 L-706125 IC50 = 196.0 nM 6.71
CHEMBL22194 L-709210 IC50 = 330.0 nM 6.48
CHEMBL282657 IC50 = 500.0 nM 6.30
CHEMBL435564 IC50 = 615.0 nM 6.21
CHEMBL283979 IC50 = 845.0 nM 6.07
CHEMBL277260 IC50 = 7500.0 nM 5.12