Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL809493

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

Binding
In vitro inhibition of binding of [125I]Bolton-Hunter SP to Tachykinin receptor 1 in human IM-9 cell line
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

Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent.
Fritz JE, Hipskind PA, Lobb KL, Nixon JA, Threlkeld PG, Gitter BD, McMillian CL, Kaldor SW.
Bioorg Med Chem Lett (2001) 11 : 1643 -1646
PubMed 11425527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.53 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42407 LANEPITANT 2.0 1 9.64
CHEMBL43044 1 9.37
CHEMBL47070 1 9.32
CHEMBL296013 1 9.19
CHEMBL42259 1 9.09
CHEMBL42191 1 9.01
CHEMBL42295 1 8.49
CHEMBL289600 1 8.48
CHEMBL42597 1 8.46
CHEMBL296216 1 8.22
CHEMBL45316 1 8.08
CHEMBL539937 1 8.01
CHEMBL434012 1 7.99
CHEMBL43970 1 7.97
CHEMBL42845 1 7.62
CHEMBL295107 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42407 LANEPITANT IC50 = 0.23 nM 9.64
CHEMBL43044 IC50 = 0.43 nM 9.37
CHEMBL47070 IC50 = 0.48 nM 9.32
CHEMBL296013 IC50 = 0.65 nM 9.19
CHEMBL42259 IC50 = 0.82 nM 9.09
CHEMBL42191 IC50 = 0.98 nM 9.01
CHEMBL42295 IC50 = 3.2 nM 8.49
CHEMBL289600 IC50 = 3.3 nM 8.48
CHEMBL42597 IC50 = 3.5 nM 8.46
CHEMBL296216 IC50 = 6.0 nM 8.22
CHEMBL45316 IC50 = 8.3 nM 8.08
CHEMBL539937 IC50 = 9.7 nM 8.01
CHEMBL434012 IC50 = 10.2 nM 7.99
CHEMBL43970 IC50 = 10.8 nM 7.97
CHEMBL42845 IC50 = 24.0 nM 7.62
CHEMBL295107 IC50 = 34.0 nM 7.47