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Assay Detail

CHEMBL839951

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

Binding
Binding affinity towards rat 5-HT7 receptor expressed in HEK cells
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 7 (CHEMBL3223)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.
Vermeulen ES, van Smeden M, Schmidt AW, Sprouse JS, Wikström HV, Grol CJ.
J Med Chem (2004) 47 : 5451 -5466
PubMed 15481983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.23 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282199 1 9.00
CHEMBL428892 1 9.00
CHEMBL12624 SB-258741 1 8.52
CHEMBL3085301 1 8.40
CHEMBL94984 1 8.00
CHEMBL187764 1 7.96
CHEMBL364124 1 7.72
CHEMBL184310 1 7.72
CHEMBL3085300 1 7.68
CHEMBL185762 1 7.28
CHEMBL188876 1 7.27
CHEMBL364795 1 7.12
CHEMBL187088 1 7.12
CHEMBL427518 1 7.00
CHEMBL364557 1 6.44
CHEMBL360382 1 6.41
CHEMBL359538 1 6.28
CHEMBL188036 1 6.25
CHEMBL366081 1 5.96
CHEMBL2051975 2 5.96
CHEMBL7220 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282199 Ki = 1.0 nM 9.00
CHEMBL428892 Ki = 1.0 nM 9.00
CHEMBL12624 SB-258741 Ki = 3.0 nM 8.52
CHEMBL3085301 Ki = 4.0 nM 8.40
CHEMBL94984 Ki = 10.0 nM 8.00
CHEMBL187764 Ki = 11.0 nM 7.96
CHEMBL364124 Ki = 19.0 nM 7.72
CHEMBL184310 Ki = 19.0 nM 7.72
CHEMBL3085300 Ki = 21.0 nM 7.68
CHEMBL185762 Ki = 52.0 nM 7.28
CHEMBL188876 Ki = 54.0 nM 7.27
CHEMBL187088 Ki = 75.0 nM 7.12
CHEMBL364795 Ki = 75.0 nM 7.12
CHEMBL427518 Ki = 100.0 nM 7.00
CHEMBL364557 Ki = 360.0 nM 6.44
CHEMBL360382 Ki = 390.0 nM 6.41
CHEMBL359538 Ki = 520.0 nM 6.28
CHEMBL188036 Ki = 560.0 nM 6.25
CHEMBL366081 Ki = 1100.0 nM 5.96
CHEMBL2051975 Ki = 1100.0 nM 5.96
CHEMBL7220 Ki = 1180.0 nM 5.93
CHEMBL2051975 Ki = 1180.0 nM 5.93