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Assay Detail

CHEMBL816613

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

Functional
Inhibition of substance P induced contraction of rabbit vena ceva (RVC) tissue expressing Tachykinin receptor 1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

3-Aryl-1,2-diacetamidopropane derivatives as novel and potent NK-1 receptor antagonists.
Hipskind PA, Howbert JJ, Bruns RF, Cho SS, Crowell TA, Foreman MM, Gehlert DR, Iyengar S, Johnson KW, Krushinski JH, Li DL, Lobb KL, Mason NR, Muehl BS, Nixon JA, Phebus LA, Regoli D, Simmons RM, Threlkeld PG, Waters DC, Gitter BD.
J Med Chem (1996) 39 : 736 -748
PubMed 8576917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.90 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16192 CP-96345 1 9.50
CHEMBL42407 LANEPITANT 2.0 1 9.40
CHEMBL351274 1 9.00
CHEMBL352102 1 6.30
CHEMBL351236 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16192 CP-96345 Kd = 0.3162 nM 9.50
CHEMBL42407 LANEPITANT Kd = 0.3981 nM 9.40
CHEMBL351274 Kd = 1.0 nM 9.00
CHEMBL352102 Kd = 501.19 nM 6.30
CHEMBL351236 Kd = 5011.87 nM 5.30