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Assay Detail

CHEMBL747299

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

Binding
Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells
15
Total Activities
15
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

Piperidine-ether based hNK1 antagonists 2: Investigation of the effect of N-substitution
Harrison T, Owens A, Williams B, Swain C, Baker R, Hutson P, Sadowski S, Cascieri M
Bioorg Med Chem Lett (1995) 5 : 209 -212
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.17 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63793 1 9.52
CHEMBL441225 CP-99994 1 9.22
CHEMBL63240 1 9.20
CHEMBL27006 1 9.06
CHEMBL27003 1 8.89
CHEMBL67667 1 8.74
CHEMBL63762 1 8.57
CHEMBL67612 1 8.55
CHEMBL432279 1 7.85
CHEMBL63257 1 7.60
CHEMBL63278 1 7.46
CHEMBL302315 1 7.17
CHEMBL292496 1 7.07
CHEMBL65153 1 6.96
CHEMBL303181 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63793 IC50 = 0.3 nM 9.52
CHEMBL441225 CP-99994 IC50 = 0.6 nM 9.22
CHEMBL63240 IC50 = 0.63 nM 9.20
CHEMBL27006 IC50 = 0.87 nM 9.06
CHEMBL27003 IC50 = 1.3 nM 8.89
CHEMBL67667 IC50 = 1.8 nM 8.74
CHEMBL63762 IC50 = 2.7 nM 8.57
CHEMBL67612 IC50 = 2.8 nM 8.55
CHEMBL432279 IC50 = 14.0 nM 7.85
CHEMBL63257 IC50 = 25.0 nM 7.60
CHEMBL63278 IC50 = 35.0 nM 7.46
CHEMBL302315 IC50 = 68.0 nM 7.17
CHEMBL292496 IC50 = 85.0 nM 7.07
CHEMBL65153 IC50 = 110.0 nM 6.96
CHEMBL303181 IC50 = 227.0 nM 6.64