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Assay Detail

CHEMBL807672

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

Binding
Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.
Perez M, Pauwels PJ, Pallard-Sigogneau I, Fourrier C, Chopin P, Palmier C, Colovray V, Halazy S.
Bioorg Med Chem Lett (1998) 8 : 3423 -3428
PubMed 9873746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.43 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113752 1 8.23
CHEMBL444794 1 8.17
CHEMBL116809 1 8.11
CHEMBL326088 1 7.80
CHEMBL115003 1 7.73
CHEMBL116626 1 7.48
CHEMBL114893 1 7.44
CHEMBL117972 1 7.34
CHEMBL113960 1 7.22
CHEMBL117405 1 6.96
CHEMBL117269 1 6.85
CHEMBL116444 1 6.81
CHEMBL117825 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113752 Ki = 5.9 nM 8.23
CHEMBL444794 Ki = 6.7 nM 8.17
CHEMBL116809 Ki = 7.8 nM 8.11
CHEMBL326088 Ki = 15.7 nM 7.80
CHEMBL115003 Ki = 18.7 nM 7.73
CHEMBL116626 Ki = 32.9 nM 7.48
CHEMBL114893 Ki = 36.4 nM 7.44
CHEMBL117972 Ki = 45.4 nM 7.34
CHEMBL113960 Ki = 60.3 nM 7.22
CHEMBL117405 Ki = 110.0 nM 6.96
CHEMBL117269 Ki = 142.0 nM 6.85
CHEMBL116444 Ki = 156.0 nM 6.81
CHEMBL117825 Ki = 391.0 nM 6.41