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Assay Detail

CHEMBL616156

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor in rat hippocampus using [3H]8-OH-DPAT
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.
Clitherow JW, Scopes DI, Skingle M, Jordan CC, Feniuk W, Campbell IB, Carter MC, Collington EW, Connor HE, Higgins GA.
J Med Chem (1994) 37 : 2253 -2257
PubMed 8057272 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.54 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL311150 1 6.60
CHEMBL306384 1 5.90
CHEMBL72700 1 5.30
CHEMBL75771 1 5.20
CHEMBL309021 1 4.70
CHEMBL72092 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL311150 Ki = 251.19 nM 6.60
CHEMBL306384 Ki = 1258.93 nM 5.90
CHEMBL72700 Ki = 5011.87 nM 5.30
CHEMBL75771 Ki = 6309.57 nM 5.20
CHEMBL309021 Ki = 19952.62 nM 4.70
CHEMBL72092 Ki < 10000.0 nM -