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Assay Detail

CHEMBL884790

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

Binding
Binding affinity towards 5-HT1A receptor using porcine cortical membrane and [3H]-8-OH-DPAT as radioligand
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents.
Hocke C, Prante O, Löber S, Hübner H, Gmeiner P, Kuwert T.
Bioorg Med Chem Lett (2005) 15 : 4819 -4823
PubMed 16139501 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.34 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL194727 1 7.82
CHEMBL198993 1 7.66
CHEMBL197214 1 7.62
CHEMBL197162 1 7.55
CHEMBL197195 1 7.52
CHEMBL194755 1 7.29
CHEMBL196744 1 7.22
CHEMBL195247 1 6.92
CHEMBL59725 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL194727 Ki = 15.0 nM 7.82
CHEMBL198993 Ki = 22.0 nM 7.66
CHEMBL197214 Ki = 24.0 nM 7.62
CHEMBL197162 Ki = 28.0 nM 7.55
CHEMBL197195 Ki = 30.0 nM 7.52
CHEMBL194755 Ki = 51.0 nM 7.29
CHEMBL196744 Ki = 60.0 nM 7.22
CHEMBL195247 Ki = 120.0 nM 6.92
CHEMBL59725 Ki = 360.0 nM 6.44