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Assay Detail

CHEMBL5371323

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 assessed as inhibition constant
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Aporphines: A privileged scaffold in CNS drug discovery.
Zhu R, Jiang G, Tang W, Zhao X, Chen F, Zhang X, Ye N.
Eur J Med Chem (2023) 256 : 115414 -115414
PubMed 37172474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.29 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25924 1 8.74
CHEMBL284586 1 7.39
CHEMBL417473 1 7.21
CHEMBL28056 1 6.85
CHEMBL283065 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25924 Ki = 1.8 nM 8.74
CHEMBL284586 Ki = 40.7 nM 7.39
CHEMBL417473 Ki = 61.5 nM 7.21
CHEMBL28056 Ki = 142.0 nM 6.85
CHEMBL283065 Ki = 554.0 nM 6.26