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Assay Detail

CHEMBL807965

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

Binding
Binding affinity towards Tachykinin receptor 1 in human IM-9 cells using [3H]-substance P as ligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type IM-9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

The discovery of (2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1- azabicyclo[2.2.2]-octan-3-amine as a novel, nonpeptide substance P antagonisst.
Lowe JA, Drozda SE, Snider RM, Longo KP, Zorn SH, Morrone J, Jackson ER, McLean S, Bryce DK, Bordner J.
J Med Chem (1992) 35 : 2591 -2600
PubMed 1378901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.17 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16192 CP-96345 1 9.11
CHEMBL346154 1 8.66
CHEMBL89652 1 7.80
CHEMBL431690 1 7.80
CHEMBL315435 1 7.78
CHEMBL86806 1 7.70
CHEMBL282331 1 7.48
CHEMBL419500 1 7.39
CHEMBL86643 1 7.17
CHEMBL86746 1 7.17
CHEMBL89897 1 6.46
CHEMBL86659 1 6.42
CHEMBL86378 1 6.31
CHEMBL433336 1 5.72
CHEMBL315176 1 4.55
CHEMBL85347 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16192 CP-96345 IC50 = 0.77 nM 9.11
CHEMBL346154 IC50 = 2.2 nM 8.66
CHEMBL89652 IC50 = 16.0 nM 7.80
CHEMBL431690 IC50 = 16.0 nM 7.80
CHEMBL315435 IC50 = 16.7 nM 7.78
CHEMBL86806 IC50 = 20.0 nM 7.70
CHEMBL282331 IC50 = 33.3 nM 7.48
CHEMBL419500 IC50 = 41.0 nM 7.39
CHEMBL86643 IC50 = 67.7 nM 7.17
CHEMBL86746 IC50 = 67.7 nM 7.17
CHEMBL89897 IC50 = 343.0 nM 6.46
CHEMBL86659 IC50 = 383.0 nM 6.42
CHEMBL86378 IC50 = 487.0 nM 6.31
CHEMBL433336 IC50 = 1890.0 nM 5.72
CHEMBL315176 IC50 = 28000.0 nM 4.55
CHEMBL85347 IC50 > 32000.0 nM -