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Assay Detail

CHEMBL816320

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Binding
Tested for binding affinity against Tachykinin receptor 2 expressed in CHO cells, using [125]SP as radioligand.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Substance-K receptor (CHEMBL2327)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.
Liu J, Underwood DJ, Cascieri MA, Rohrer SP, Cantin LD, Chicchi G, Smith AB, Hirschmann R.
J Med Chem (2000) 43 : 3827 -3831
PubMed 11052787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.78 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112246 1 7.57
CHEMBL2112245 1 7.34
CHEMBL2369630 1 6.14
CHEMBL2369631 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112246 IC50 = 27.0 nM 7.57
CHEMBL2112245 IC50 = 46.0 nM 7.34
CHEMBL2369630 IC50 = 730.0 nM 6.14
CHEMBL2369631 IC50 = 850.0 nM 6.07