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Assay Detail

CHEMBL1024699

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

Binding
Displacement of [3H]substance P from human NK1 receptor expressed in CHO cell membrane by liquid scintillation counting
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Yamamoto T, Nair P, Jacobsen NE, Davis P, Ma SW, Navratilova E, Moye S, Lai J, Yamamura HI, Vanderah TW, Porreca F, Hruby VJ.
J Med Chem (2008) 51 : 6334 -6347
PubMed 18821747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.24 10.08
IC50 4 9.50 10.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL507340 2 10.90
CHEMBL389652 2 10.08
CHEMBL22870 L-732138 2 9.14
CHEMBL448998 2 8.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL507340 IC50 = 0.01259 nM 10.90
CHEMBL389652 Ki = 0.084 nM 10.08
CHEMBL389652 IC50 = 0.1259 nM 9.90
CHEMBL22870 L-732138 Ki = 0.73 nM 9.14
CHEMBL22870 L-732138 IC50 = 1.585 nM 8.80
CHEMBL448998 Ki = 3.2 nM 8.49
CHEMBL448998 IC50 = 3.981 nM 8.40
CHEMBL507340 Ki = 0.0065 nM -