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Assay Detail

CHEMBL804074

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Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 5A (CHEMBL3426)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D3 receptor preference and improved pharmacokinetic properties
Haadsma-Svensson SR, Smith MW, Lin C, Neil Duncan J, Sonesson C, Wikstrom H, Waters N, Carlsson A, Svensson K
Bioorg Med Chem Lett (1994) 4 : 689 -694
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.12 6.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278751 1 6.78
CHEMBL161507 1 6.54
CHEMBL27441 1 5.63
CHEMBL349843 1 5.51
CHEMBL161811 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278751 Ki = 168.0 nM 6.78
CHEMBL161507 Ki = 287.0 nM 6.54
CHEMBL27441 Ki = 2331.0 nM 5.63
CHEMBL349843 Ki = 3067.0 nM 5.51
CHEMBL161811 Ki > 3448.0 nM -