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Assay Detail

CHEMBL961641

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

Binding
Inhibition of human 5HT7 receptor expressed in HEK293 cells by competitive binding assay
23
Total Activities
23
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 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: synthesis and biological evaluation.
Badarau E, Suzenet F, Bojarski AJ, Fînaru AL, Guillaumet G.
Bioorg Med Chem Lett (2009) 19 : 1600 -1603
PubMed 19237285 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.77 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL177064 1 8.37
CHEMBL515780 1 8.22
CHEMBL515939 1 8.15
CHEMBL479105 1 7.96
CHEMBL478905 1 7.70
CHEMBL476463 1 7.58
CHEMBL476464 1 7.42
CHEMBL478680 1 7.40
CHEMBL476462 1 7.32
CHEMBL518752 1 7.11
CHEMBL476616 1 6.78
CHEMBL478682 1 6.61
CHEMBL476821 1 6.57
CHEMBL476615 1 6.53
CHEMBL477065 1 6.25
CHEMBL476862 1 6.06
CHEMBL478073 1 6.04
CHEMBL514058 1 5.99
CHEMBL476248 1 5.91
CHEMBL476822 1 5.74
CHEMBL477066 1 5.73
CHEMBL515783 1 5.60
CHEMBL515789 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL177064 Ki = 4.3 nM 8.37
CHEMBL515780 Ki = 6.0 nM 8.22
CHEMBL515939 Ki = 7.0 nM 8.15
CHEMBL479105 Ki = 11.0 nM 7.96
CHEMBL478905 Ki = 20.0 nM 7.70
CHEMBL476463 Ki = 26.0 nM 7.58
CHEMBL476464 Ki = 38.0 nM 7.42
CHEMBL478680 Ki = 40.0 nM 7.40
CHEMBL476462 Ki = 48.0 nM 7.32
CHEMBL518752 Ki = 78.0 nM 7.11
CHEMBL476616 Ki = 168.0 nM 6.78
CHEMBL478682 Ki = 243.0 nM 6.61
CHEMBL476821 Ki = 267.0 nM 6.57
CHEMBL476615 Ki = 296.0 nM 6.53
CHEMBL477065 Ki = 566.0 nM 6.25
CHEMBL476862 Ki = 864.0 nM 6.06
CHEMBL478073 Ki = 902.0 nM 6.04
CHEMBL514058 Ki = 1029.0 nM 5.99
CHEMBL476248 Ki = 1230.0 nM 5.91
CHEMBL476822 Ki = 1838.0 nM 5.74
CHEMBL477066 Ki = 1867.0 nM 5.73
CHEMBL515783 Ki = 2500.0 nM 5.60
CHEMBL515789 Ki = 17960.0 nM 4.75