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Assay Detail

CHEMBL616305

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

Binding
Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue using [3H]OH-DPAT as radioligand.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of propranolol analogues as serotonergic agents.
Pierson ME, Lyon RA, Titeler M, Schulman SB, Kowalski P, Glennon RA.
J Med Chem (1989) 32 : 859 -863
PubMed 2539480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.45 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138907 1 7.41
CHEMBL140417 1 7.35
CHEMBL452861 LEVOPROPRANOLOL 2.0 1 7.26
CHEMBL337539 1 7.22
CHEMBL139103 1 7.10
CHEMBL27 PROPRANOLOL 4.0 1 7.05
CHEMBL140416 1 7.02
CHEMBL334465 1 6.82
CHEMBL169956 1 6.65
CHEMBL138136 1 6.46
CHEMBL136470 1 6.40
CHEMBL367935 1 6.35
CHEMBL275742 DEXPROPRANOLOL 2.0 1 5.77
CHEMBL168635 1 5.56
CHEMBL168224 1 5.52
CHEMBL138509 1 5.48
CHEMBL170845 1 5.31
CHEMBL136072 1 5.31
CHEMBL139976 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138907 Ki = 39.0 nM 7.41
CHEMBL140417 Ki = 45.0 nM 7.35
CHEMBL452861 LEVOPROPRANOLOL Ki = 55.0 nM 7.26
CHEMBL337539 Ki = 60.0 nM 7.22
CHEMBL139103 Ki = 80.0 nM 7.10
CHEMBL27 PROPRANOLOL Ki = 90.0 nM 7.05
CHEMBL140416 Ki = 95.0 nM 7.02
CHEMBL334465 Ki = 150.0 nM 6.82
CHEMBL169956 Ki = 225.0 nM 6.65
CHEMBL138136 Ki = 345.0 nM 6.46
CHEMBL136470 Ki = 400.0 nM 6.40
CHEMBL367935 Ki = 450.0 nM 6.35
CHEMBL275742 DEXPROPRANOLOL Ki = 1700.0 nM 5.77
CHEMBL168635 Ki = 2750.0 nM 5.56
CHEMBL168224 Ki = 3000.0 nM 5.52
CHEMBL138509 Ki = 3300.0 nM 5.48
CHEMBL170845 Ki = 4900.0 nM 5.31
CHEMBL136072 Ki = 4850.0 nM 5.31
CHEMBL139976 Ki > 25000.0 nM -