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Assay Detail

CHEMBL1024700

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

Binding
Displacement of [3H]substance P from rat 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 Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Substance-P receptor (CHEMBL4027)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 7.68 9.54
IC50 4 7.15 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL389652 2 9.54
CHEMBL507340 2 8.14
CHEMBL22870 L-732138 2 6.89
CHEMBL448998 2 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL389652 Ki = 0.29 nM 9.54
CHEMBL389652 IC50 = 1.0 nM 9.00
CHEMBL507340 Ki = 7.3 nM 8.14
CHEMBL507340 IC50 = 25.12 nM 7.60
CHEMBL22870 L-732138 Ki = 130.0 nM 6.89
CHEMBL22870 L-732138 IC50 = 398.11 nM 6.40
CHEMBL448998 Ki = 700.0 nM 6.16
CHEMBL448998 IC50 = 2511.89 nM 5.60