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Assay Detail

CHEMBL749477

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Binding
Tested for the inhibitory potency against Neurokinin 1 NK1 receptor
6
Total Activities
5
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

Studies on the active conformation of NK1 antagonist CGP 49823. Part 1. Synthesis of conformationally restricted analogs.
Veenstra SJ, Hauser K, Betschart C
Bioorg Med Chem Lett (1997) 7 : 347 -350
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.77 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290364 1 7.92
CHEMBL332111 1 7.52
CHEMBL419232 2 7.36
CHEMBL119025 1 6.00
CHEMBL333726 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290364 IC50 = 12.0 nM 7.92
CHEMBL332111 IC50 = 30.0 nM 7.52
CHEMBL419232 IC50 = 44.0 nM 7.36
CHEMBL419232 IC50 = 640.0 nM 6.19
CHEMBL119025 IC50 = 1000.0 nM 6.00
CHEMBL333726 IC50 = 2300.0 nM 5.64