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Assay Detail

CHEMBL828758

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

Binding
Binding affinity toward 5-HT2B receptor evaluated by displacement of [3H]5-HT radioligand
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.
Röver S, Adams DR, Bénardeau A, Bentley JM, Bickerdike MJ, Bourson A, Cliffe IA, Coassolo P, Davidson JE, Dourish CT, Hebeisen P, Kennett GA, Knight AR, Malcolm CS, Mattei P, Misra A, Mizrahi J, Muller M, Porter RH, Richter H, Taylor S, Vickers SP.
Bioorg Med Chem Lett (2005) 15 : 3604 -3608
PubMed 15975787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.22 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190699 1 8.49
CHEMBL187739 1 8.00
CHEMBL361079 1 7.96
CHEMBL188033 1 7.89
CHEMBL2112055 1 7.82
CHEMBL191054 1 7.72
CHEMBL190124 1 7.68
CHEMBL188605 1 7.28
CHEMBL190584 1 7.23
CHEMBL364534 1 7.17
CHEMBL187888 1 7.05
CHEMBL425545 1 6.85
CHEMBL2096809 2 6.80
CHEMBL361929 1 6.60
CHEMBL187787 1 6.02
CHEMBL2096711 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190699 Ki = 3.2 nM 8.49
CHEMBL187739 Ki = 10.0 nM 8.00
CHEMBL361079 Ki = 11.0 nM 7.96
CHEMBL188033 Ki = 13.0 nM 7.89
CHEMBL2112055 Ki = 15.0 nM 7.82
CHEMBL191054 Ki = 19.0 nM 7.72
CHEMBL190124 Ki = 21.0 nM 7.68
CHEMBL188605 Ki = 53.0 nM 7.28
CHEMBL190584 Ki = 59.0 nM 7.23
CHEMBL364534 Ki = 67.0 nM 7.17
CHEMBL187888 Ki = 90.0 nM 7.05
CHEMBL425545 Ki = 140.0 nM 6.85
CHEMBL2096809 Ki = 160.0 nM 6.80
CHEMBL2096809 Ki = 210.0 nM 6.68
CHEMBL361929 Ki = 250.0 nM 6.60
CHEMBL187787 Ki = 960.0 nM 6.02
CHEMBL2096711 Ki = 2600.0 nM 5.58