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Assay Detail

CHEMBL748488

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

Binding
Displacement of [125I]-substance P from hNK1 receptor in chinese hamster ovarian (CHO) cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.
Elliott JM, Broughton H, Cascieri MA, Chicchi G, Huscroft IT, Kurtz M, MacLeod AM, Sadowski S, Stevenson GI.
Bioorg Med Chem Lett (1998) 8 : 1851 -1856
PubMed 9873446 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53312 1 9.00
CHEMBL292190 1 8.32
CHEMBL53314 1 7.89
CHEMBL405820 1 7.77
CHEMBL299528 1 7.21
CHEMBL417026 1 6.58
CHEMBL299312 1 6.48
CHEMBL54931 1 6.42
CHEMBL297957 1 6.26
CHEMBL52198 1 6.25
CHEMBL299089 1 6.22
CHEMBL55691 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53312 IC50 = 1.0 nM 9.00
CHEMBL292190 IC50 = 4.8 nM 8.32
CHEMBL53314 IC50 = 13.0 nM 7.89
CHEMBL405820 IC50 = 17.0 nM 7.77
CHEMBL299528 IC50 = 61.0 nM 7.21
CHEMBL417026 IC50 = 263.0 nM 6.58
CHEMBL299312 IC50 = 330.0 nM 6.48
CHEMBL54931 IC50 = 382.0 nM 6.42
CHEMBL297957 IC50 = 547.0 nM 6.26
CHEMBL52198 IC50 = 558.0 nM 6.25
CHEMBL299089 IC50 = 602.0 nM 6.22
CHEMBL55691 IC50 = 2500.0 nM 5.60