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Assay Detail

CHEMBL813323

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

Binding
Binding affinity towards Tachykinin receptor 1 in rat cerebral cortex membranes was determined by using 125 [I]-BHSP as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Substance-P receptor (CHEMBL4027)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

An SAR study for the non-peptide substance P receptor (NK1) antagonist, CP-96,345.
Howson W, Hodgson J, Richardson R, Walton L, Guard S, Watling K
Bioorg Med Chem Lett (1992) 2 : 559 -564
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.70 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235363 SUBSTANCE P 1.0 1 9.92
CHEMBL217406 NEUROKININ A 1 7.51
CHEMBL437797 NEUROKININ B 1 7.16
CHEMBL356912 1 6.96
CHEMBL346154 1 6.92
CHEMBL346633 1 6.16
CHEMBL345711 1 6.13
CHEMBL419500 1 6.10
CHEMBL152239 1 6.00
CHEMBL357717 1 5.70
CHEMBL153042 1 5.14
CHEMBL358033 1 -
CHEMBL449347 1 -
CHEMBL152011 1 -
CHEMBL152055 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235363 SUBSTANCE P IC50 = 0.12 nM 9.92
CHEMBL217406 NEUROKININ A IC50 = 31.0 nM 7.51
CHEMBL437797 NEUROKININ B IC50 = 69.0 nM 7.16
CHEMBL356912 IC50 = 110.0 nM 6.96
CHEMBL346154 IC50 = 120.0 nM 6.92
CHEMBL346633 IC50 = 700.0 nM 6.16
CHEMBL345711 IC50 = 740.0 nM 6.13
CHEMBL419500 IC50 = 800.0 nM 6.10
CHEMBL152239 IC50 = 990.0 nM 6.00
CHEMBL357717 IC50 = 2000.0 nM 5.70
CHEMBL153042 IC50 = 7200.0 nM 5.14
CHEMBL358033 IC50 > 10000.0 nM -
CHEMBL449347 IC50 ~ 10000.0 nM -
CHEMBL152011 IC50 > 1000.0 nM -
CHEMBL152055 IC50 > 10000.0 nM -