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Assay Detail

CHEMBL4308345

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

Binding
Displacement of [3H]-8-OH-DPAT from full length human cloned 5HT1A receptor expressed in HEK293 cells incubated for 1 hr by radioligand displacement assay
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

Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.
Kułaga D, Jaśkowska J, Satała G.
Bioorg Med Chem Lett (2019) 29 : 126667 -126667
PubMed 31547945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.51 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4434735 1 8.40
CHEMBL4454105 1 8.05
CHEMBL4473026 1 7.92
CHEMBL4592941 1 7.89
CHEMBL4456046 1 7.72
CHEMBL4540404 1 7.70
CHEMBL4464512 1 7.68
CHEMBL4440695 1 7.64
CHEMBL4470487 1 7.62
CHEMBL4463030 1 7.60
CHEMBL4457109 1 7.58
CHEMBL4465181 1 7.27
CHEMBL4569757 1 7.24
CHEMBL4439795 1 7.08
CHEMBL4565558 1 7.04
CHEMBL4462839 1 6.81
CHEMBL4439144 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4434735 Ki = 4.0 nM 8.40
CHEMBL4454105 Ki = 9.0 nM 8.05
CHEMBL4473026 Ki = 12.0 nM 7.92
CHEMBL4592941 Ki = 13.0 nM 7.89
CHEMBL4456046 Ki = 19.0 nM 7.72
CHEMBL4540404 Ki = 20.0 nM 7.70
CHEMBL4464512 Ki = 21.0 nM 7.68
CHEMBL4440695 Ki = 23.0 nM 7.64
CHEMBL4470487 Ki = 24.0 nM 7.62
CHEMBL4463030 Ki = 25.0 nM 7.60
CHEMBL4457109 Ki = 26.0 nM 7.58
CHEMBL4465181 Ki = 54.0 nM 7.27
CHEMBL4569757 Ki = 58.0 nM 7.24
CHEMBL4439795 Ki = 84.0 nM 7.08
CHEMBL4565558 Ki = 91.0 nM 7.04
CHEMBL4462839 Ki = 156.0 nM 6.81
CHEMBL4439144 Ki = 327.0 nM 6.49