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Assay Detail

CHEMBL1217615

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

Binding
Displacement of [3H]substance P frome rat NK2 receptor
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Substance-K receptor (CHEMBL4554)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing two penicillamines.
Yamamoto T, Nair P, Jacobsen NE, Kulkarni V, Davis P, Ma SW, Navratilova E, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.
J Med Chem (2010) 53 : 5491 -5501
PubMed 20617791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.62 8.35
IC50 6 7.05 7.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1214025 2 8.35
CHEMBL507340 2 8.14
CHEMBL1214024 2 8.00
CHEMBL1214027 2 7.58
CHEMBL22870 L-732138 2 6.87
CHEMBL1214026 2 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1214025 Ki = 4.5 nM 8.35
CHEMBL507340 Ki = 7.3 nM 8.14
CHEMBL1214024 Ki = 10.0 nM 8.00
CHEMBL1214025 IC50 = 18.2 nM 7.74
CHEMBL507340 IC50 = 24.55 nM 7.61
CHEMBL1214027 Ki = 26.0 nM 7.58
CHEMBL1214024 IC50 = 41.69 nM 7.38
CHEMBL1214027 IC50 = 104.71 nM 6.98
CHEMBL22870 L-732138 Ki = 134.0 nM 6.87
CHEMBL1214026 Ki = 160.0 nM 6.80
CHEMBL22870 L-732138 IC50 = 398.11 nM 6.40
CHEMBL1214026 IC50 = 660.69 nM 6.18