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Assay Detail

CHEMBL824640

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

Binding
Displacement of [125 I]-[MePhe]-NKB binding to hNK-3-CHO (Chinese hamster ovary) membranes
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuromedin-K receptor (CHEMBL4429)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.
Blaney FE, Raveglia LF, Artico M, Cavagnera S, Dartois C, Farina C, Grugni M, Gagliardi S, Luttmann MA, Martinelli M, Nadler GM, Parini C, Petrillo P, Sarau HM, Scheideler MA, Hay DW, Giardina GA.
J Med Chem (2001) 44 : 1675 -1689
PubMed 11356103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.13 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45129 1 9.10
CHEMBL33868 1 8.92
CHEMBL296857 1 8.92
CHEMBL45961 1 8.85
CHEMBL10188 TALNETANT 2.0 1 8.85
CHEMBL47544 1 8.82
CHEMBL47739 1 8.77
CHEMBL47713 1 8.74
CHEMBL47775 1 8.72
CHEMBL44722 1 8.66
CHEMBL295059 1 8.48
CHEMBL47412 1 8.47
CHEMBL47179 1 8.34
CHEMBL47408 1 8.33
CHEMBL47275 1 8.15
CHEMBL432301 1 7.51
CHEMBL295770 1 6.71
CHEMBL296122 1 6.34
CHEMBL297086 1 5.92
CHEMBL45362 1 5.90
CHEMBL47555 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45129 Ki = 0.8 nM 9.10
CHEMBL33868 Ki = 1.2 nM 8.92
CHEMBL296857 Ki = 1.2 nM 8.92
CHEMBL45961 Ki = 1.4 nM 8.85
CHEMBL10188 TALNETANT Ki = 1.4 nM 8.85
CHEMBL47544 Ki = 1.5 nM 8.82
CHEMBL47739 Ki = 1.7 nM 8.77
CHEMBL47713 Ki = 1.8 nM 8.74
CHEMBL47775 Ki = 1.9 nM 8.72
CHEMBL44722 Ki = 2.2 nM 8.66
CHEMBL295059 Ki = 3.3 nM 8.48
CHEMBL47412 Ki = 3.4 nM 8.47
CHEMBL47179 Ki = 4.6 nM 8.34
CHEMBL47408 Ki = 4.7 nM 8.33
CHEMBL47275 Ki = 7.0 nM 8.15
CHEMBL432301 Ki = 31.2 nM 7.51
CHEMBL295770 Ki = 193.0 nM 6.71
CHEMBL296122 Ki = 454.0 nM 6.34
CHEMBL297086 Ki = 1210.0 nM 5.92
CHEMBL45362 Ki = 1250.0 nM 5.90
CHEMBL47555 Ki > 12000.0 nM -