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Assay Detail

CHEMBL818108

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Binding
Displacement of [125 I]-NKA binding to tachykinin receptor 2 in CHO 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

Substance-K receptor (CHEMBL2327)
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 8.06 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL47739 1 9.22
CHEMBL47775 1 9.15
CHEMBL45129 1 9.10
CHEMBL295770 1 9.00
CHEMBL45961 1 8.92
CHEMBL296857 1 8.82
CHEMBL33868 1 8.80
CHEMBL47412 1 8.62
CHEMBL45362 1 8.38
CHEMBL47544 1 8.34
CHEMBL47713 1 8.24
CHEMBL47179 1 8.21
CHEMBL296122 1 8.04
CHEMBL297086 1 7.73
CHEMBL47408 1 7.65
CHEMBL432301 1 7.48
CHEMBL295059 1 7.29
CHEMBL10188 TALNETANT 2.0 1 6.84
CHEMBL44722 1 6.76
CHEMBL47275 1 6.56
CHEMBL47555 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL47739 Ki = 0.6 nM 9.22
CHEMBL47775 Ki = 0.7 nM 9.15
CHEMBL45129 Ki = 0.8 nM 9.10
CHEMBL295770 Ki = 1.0 nM 9.00
CHEMBL45961 Ki = 1.2 nM 8.92
CHEMBL296857 Ki = 1.5 nM 8.82
CHEMBL33868 Ki = 1.6 nM 8.80
CHEMBL47412 Ki = 2.4 nM 8.62
CHEMBL45362 Ki = 4.2 nM 8.38
CHEMBL47544 Ki = 4.6 nM 8.34
CHEMBL47713 Ki = 5.7 nM 8.24
CHEMBL47179 Ki = 6.1 nM 8.21
CHEMBL296122 Ki = 9.2 nM 8.04
CHEMBL297086 Ki = 18.5 nM 7.73
CHEMBL47408 Ki = 22.2 nM 7.65
CHEMBL432301 Ki = 33.0 nM 7.48
CHEMBL295059 Ki = 51.6 nM 7.29
CHEMBL10188 TALNETANT Ki = 144.0 nM 6.84
CHEMBL44722 Ki = 172.0 nM 6.76
CHEMBL47275 Ki = 276.0 nM 6.56
CHEMBL47555 Ki = 811.0 nM 6.09