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Assay Detail

CHEMBL616582

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

Binding
The compound was tested for binding affinity on [3H]8-OH-DPAT as specific ligand on 5-hydroxytryptamine 1A receptor in rat hippocampus
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.
Barlocco D, Cignarella G, Montesano F, Leonardi A, Mella M, Toma L.
J Med Chem (1999) 42 : 173 -177
PubMed 9888842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.31 8.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 8.63
CHEMBL301078 1 7.79
CHEMBL51074 1 7.67
CHEMBL49851 1 7.25
CHEMBL301726 1 6.91
CHEMBL2 PRAZOSIN 4.0 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 2.33 nM 8.63
CHEMBL301078 Ki = 16.3 nM 7.79
CHEMBL51074 Ki = 21.2 nM 7.67
CHEMBL49851 Ki = 56.5 nM 7.25
CHEMBL301726 Ki = 123.0 nM 6.91
CHEMBL2 PRAZOSIN Ki = 2360.0 nM 5.63