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Assay Detail

CHEMBL745040

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

Binding
Displacement of [125]Substance P Binding from human Neurokinin NK1 receptor in CHO Cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Quinuclidine-based NK-1 antagonists I: 3-benzyloxy-1-azabicyclo[2.2.2]octanes
Seward EM, Swain CJ, Merchant KJ, Owen SN, Sabin V, Cascieri MA, Sadowski S, Strader C, Baker R
Bioorg Med Chem Lett (1993) 3 : 1361 -1366
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.36 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16192 CP-96345 1 9.30
CHEMBL283356 L-706125 1 9.00
CHEMBL280849 1 7.68
CHEMBL29487 1 7.32
CHEMBL431690 1 6.82
CHEMBL29293 1 6.74
CHEMBL429610 1 6.71
CHEMBL30139 1 6.54
CHEMBL282996 1 6.16
CHEMBL29993 1 -
CHEMBL287674 1 -
CHEMBL29785 1 -
CHEMBL281502 1 -
CHEMBL29760 1 -
CHEMBL281703 1 -
CHEMBL29786 1 -
CHEMBL30029 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16192 CP-96345 IC50 = 0.5 nM 9.30
CHEMBL283356 L-706125 IC50 = 1.0 nM 9.00
CHEMBL280849 IC50 = 21.0 nM 7.68
CHEMBL29487 IC50 = 48.0 nM 7.32
CHEMBL431690 IC50 = 150.0 nM 6.82
CHEMBL29293 IC50 = 183.0 nM 6.74
CHEMBL429610 IC50 = 197.0 nM 6.71
CHEMBL30139 IC50 = 290.0 nM 6.54
CHEMBL282996 IC50 = 700.0 nM 6.16
CHEMBL29993 IC50 > 1000.0 nM -
CHEMBL287674 IC50 > 1000.0 nM -
CHEMBL29785 IC50 > 1000.0 nM -
CHEMBL281502 IC50 > 1000.0 nM -
CHEMBL29760 IC50 > 1000.0 nM -
CHEMBL281703 IC50 > 1000.0 nM -
CHEMBL29786 IC50 > 1000.0 nM -
CHEMBL30029 IC50 = 110000.0 nM -