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Assay Detail

CHEMBL873471

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Binding
Binding affinity was measured against the Tachykinin receptor 1 in bovine retina using [3H]SP
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Substance-P receptor (CHEMBL249)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Derivation of a three-dimensional pharmacophore model of substance P antagonists bound to the neurokinin-1 receptor.
Takeuchi Y, Shands EF, Beusen DD, Marshall GR.
J Med Chem (1998) 41 : 3609 -3623
PubMed 9733486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.68 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121852 1 7.82
CHEMBL118565 1 7.59
CHEMBL120190 1 7.52
CHEMBL101420 1 6.51
CHEMBL289573 1 5.86
CHEMBL297134 1 5.86
CHEMBL102525 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121852 IC50 = 15.14 nM 7.82
CHEMBL118565 IC50 = 25.7 nM 7.59
CHEMBL120190 IC50 = 30.2 nM 7.52
CHEMBL101420 IC50 = 309.03 nM 6.51
CHEMBL289573 IC50 = 1380.38 nM 5.86
CHEMBL297134 IC50 = 1380.38 nM 5.86
CHEMBL102525 IC50 = 2691.53 nM 5.57