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Assay Detail

CHEMBL812544

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Binding
Binding affinity towards Tachykinin receptor 1
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.
Hirschmann R, Yao W, Cascieri MA, Strader CD, Maechler L, Cichy-Knight MA, Hynes J, van Rijn RD, Sprengeler PA, Smith AB.
J Med Chem (1996) 39 : 2441 -2448
PubMed 8691440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.99 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420221 1 7.22
CHEMBL281200 1 6.75
CHEMBL282618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420221 IC50 = 60.0 nM 7.22
CHEMBL281200 IC50 = 180.0 nM 6.75
CHEMBL282618 IC50 = 120000.0 nM -