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Assay Detail

CHEMBL4148418

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

Binding
Displacement of [3H]-8-OH-DPAT from human 5HT1AR expressed in HEK293 cell membranes after 1 hr by Microbeta scintillation counting method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT7 receptor agents with antidepressant activity.
Kucwaj-Brysz K, Kurczab R, Jastrzębska-Więsek M, Żesławska E, Satała G, Nitek W, Partyka A, Siwek A, Jankowska A, Wesołowska A, Kieć-Kononowicz K, Handzlik J.
Eur J Med Chem (2018) 147 : 102 -114
PubMed 29425815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.48 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49 BUSPIRONE 4.0 1 7.70
CHEMBL4170657 1 7.07
CHEMBL4163778 1 7.00
CHEMBL4166804 1 7.00
CHEMBL4159967 1 6.96
CHEMBL4170613 1 6.85
CHEMBL4176588 1 6.74
CHEMBL4176950 1 6.72
CHEMBL4170484 1 6.71
CHEMBL4171652 1 6.66
CHEMBL4174055 1 6.52
CHEMBL4162548 1 6.47
CHEMBL4168743 1 6.38
CHEMBL4162279 1 6.23
CHEMBL4163626 1 5.65
CHEMBL4174681 1 4.74
CHEMBL4160262 1 4.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49 BUSPIRONE Ki = 20.0 nM 7.70
CHEMBL4170657 Ki = 85.0 nM 7.07
CHEMBL4163778 Ki = 100.0 nM 7.00
CHEMBL4166804 Ki = 99.0 nM 7.00
CHEMBL4159967 Ki = 109.0 nM 6.96
CHEMBL4170613 Ki = 140.0 nM 6.85
CHEMBL4176588 Ki = 184.0 nM 6.74
CHEMBL4176950 Ki = 190.0 nM 6.72
CHEMBL4170484 Ki = 197.0 nM 6.71
CHEMBL4171652 Ki = 219.0 nM 6.66
CHEMBL4174055 Ki = 305.0 nM 6.52
CHEMBL4162548 Ki = 341.0 nM 6.47
CHEMBL4168743 Ki = 421.0 nM 6.38
CHEMBL4162279 Ki = 585.0 nM 6.23
CHEMBL4163626 Ki = 2249.0 nM 5.65
CHEMBL4174681 Ki = 18290.0 nM 4.74
CHEMBL4160262 Ki = 18430.0 nM 4.73