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Assay Detail

CHEMBL2037806

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

Binding
Displacement of [3H]8-OH-DPAT from human 5HT1A receptor by liquid scintillation counting
23
Total Activities
23
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

Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.
Zhu XY, Etukala JR, Eyunni SV, Setola V, Roth BL, Ablordeppey SY.
Eur J Med Chem (2012) 53 : 124 -132
PubMed 22520153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.29 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.52
CHEMBL2037530 1 8.44
CHEMBL2037529 1 8.44
CHEMBL2037522 1 8.29
CHEMBL2037521 1 8.18
CHEMBL2037531 1 8.14
CHEMBL2037528 1 7.55
CHEMBL2037519 1 7.20
CHEMBL2037518 1 7.07
CHEMBL2037431 1 7.04
CHEMBL2037526 1 6.99
CHEMBL2037523 1 6.96
CHEMBL2037527 1 6.67
CHEMBL1946255 1 6.67
CHEMBL2037520 1 6.60
CHEMBL1946254 1 6.58
CHEMBL2037430 1 6.51
CHEMBL2037525 1 6.46
CHEMBL1946257 1 6.30
CHEMBL2037432 1 6.11
CHEMBL1946258 1 -
CHEMBL2037524 1 -
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE Ki = 0.3 nM 9.52
CHEMBL2037530 Ki = 3.6 nM 8.44
CHEMBL2037529 Ki = 3.6 nM 8.44
CHEMBL2037522 Ki = 5.1 nM 8.29
CHEMBL2037521 Ki = 6.6 nM 8.18
CHEMBL2037531 Ki = 7.3 nM 8.14
CHEMBL2037528 Ki = 28.3 nM 7.55
CHEMBL2037519 Ki = 63.0 nM 7.20
CHEMBL2037518 Ki = 85.0 nM 7.07
CHEMBL2037431 Ki = 90.5 nM 7.04
CHEMBL2037526 Ki = 103.0 nM 6.99
CHEMBL2037523 Ki = 111.0 nM 6.96
CHEMBL2037527 Ki = 214.0 nM 6.67
CHEMBL1946255 Ki = 216.0 nM 6.67
CHEMBL2037520 Ki = 252.0 nM 6.60
CHEMBL1946254 Ki = 263.0 nM 6.58
CHEMBL2037430 Ki = 312.0 nM 6.51
CHEMBL2037525 Ki = 350.0 nM 6.46
CHEMBL1946257 Ki = 495.0 nM 6.30
CHEMBL2037432 Ki = 771.0 nM 6.11
CHEMBL1946258 Ki - -
CHEMBL2037524 Ki > 10000.0 nM -
CHEMBL1201082 FLUOXETINE HYDROCHLORIDE Ki - -