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Assay Detail

CHEMBL750303

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

Functional
Tested for antagonist activity at NK-2 tachykinin receptors in hamster trachea
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cricetulus griseus
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Substance-K receptor (CHEMBL2304405)
Type SINGLE PROTEIN
Organism Mesocricetus auratus

Publication

Influence of lipophilicity on the biological activity of cyclic pseudopeptide NK-2 receptor antagonists.
Quartara L, Fabbri G, Ricci R, Patacchini R, Pestellini V, Maggi CA, Pavone V, Giachetti A, Arcamone F.
J Med Chem (1994) 37 : 3630 -3638
PubMed 7932590 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 15 7.95 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334186 1 9.26
CHEMBL433191 1 9.06
CHEMBL121271 1 8.79
CHEMBL331480 1 8.66
CHEMBL333515 1 8.42
CHEMBL427606 1 8.39
CHEMBL333027 1 8.17
CHEMBL121571 1 7.89
CHEMBL421062 1 7.80
CHEMBL330810 1 7.73
CHEMBL421071 1 7.50
CHEMBL332872 1 7.17
CHEMBL384610 1 7.00
CHEMBL433192 1 6.96
CHEMBL332820 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334186 Kd = 0.5495 nM 9.26
CHEMBL433191 Kd = 0.871 nM 9.06
CHEMBL121271 Kd = 1.622 nM 8.79
CHEMBL331480 Kd = 2.188 nM 8.66
CHEMBL333515 Kd = 3.802 nM 8.42
CHEMBL427606 Kd = 4.074 nM 8.39
CHEMBL333027 Kd = 6.761 nM 8.17
CHEMBL121571 Kd = 12.88 nM 7.89
CHEMBL421062 Kd = 15.85 nM 7.80
CHEMBL330810 Kd = 18.62 nM 7.73
CHEMBL421071 Kd = 31.62 nM 7.50
CHEMBL332872 Kd = 67.61 nM 7.17
CHEMBL384610 Kd = 100.0 nM 7.00
CHEMBL433192 Kd = 109.65 nM 6.96
CHEMBL332820 Kd = 309.03 nM 6.51