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Assay Detail

CHEMBL818003

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Binding
Binding affinity towards Tachykinin receptor 2
16
Total Activities
16
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

Discovery of potent cyclic pseudopeptide human tachykinin NK-2 receptor antagonists.
Giannotti D, Perrotta E, Di Bugno C, Nannicini R, Harmat NJ, Giolitti A, Patacchini R, Renzetti AR, Rotondaro L, Giuliani S, Altamura M, Maggi CA.
J Med Chem (2000) 43 : 4041 -4044
PubMed 11063600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.47 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223221 1 10.00
CHEMBL334721 1 9.20
CHEMBL323884 1 8.80
CHEMBL435324 1 8.70
CHEMBL407782 1 8.60
CHEMBL116564 1 8.10
CHEMBL336053 1 8.00
CHEMBL263194 1 8.00
CHEMBL2112675 1 7.70
CHEMBL114442 1 6.50
CHEMBL337628 1 6.20
CHEMBL114036 1 6.10
CHEMBL131024 1 5.90
CHEMBL2111858 1 5.90
CHEMBL324804 1 5.90
CHEMBL2112669 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223221 Ki = 0.1 nM 10.00
CHEMBL334721 Ki = 0.631 nM 9.20
CHEMBL323884 Ki = 1.585 nM 8.80
CHEMBL435324 Ki = 1.995 nM 8.70
CHEMBL407782 Ki = 2.512 nM 8.60
CHEMBL116564 Ki = 7.943 nM 8.10
CHEMBL336053 Ki = 10.0 nM 8.00
CHEMBL263194 Ki = 10.0 nM 8.00
CHEMBL2112675 Ki = 19.95 nM 7.70
CHEMBL114442 Ki = 316.23 nM 6.50
CHEMBL337628 Ki = 630.96 nM 6.20
CHEMBL114036 Ki = 794.33 nM 6.10
CHEMBL131024 Ki = 1258.93 nM 5.90
CHEMBL2111858 Ki = 1258.93 nM 5.90
CHEMBL324804 Ki = 1258.93 nM 5.90
CHEMBL2112669 Ki = 1258.93 nM 5.90