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Assay Detail

CHEMBL861244

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

Binding
Displacement of [3H]5HT from human recombinant 5HT2C receptor expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.
Richter HG, Adams DR, Benardeau A, Bickerdike MJ, Bentley JM, Blench TJ, Cliffe IA, Dourish C, Hebeisen P, Kennett GA, Knight AR, Malcolm CS, Mattei P, Misra A, Mizrahi J, Monck NJ, Plancher JM, Roever S, Roffey JR, Taylor S, Vickers SP.
Bioorg Med Chem Lett (2006) 16 : 1207 -1211
PubMed 16361098 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.95 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190699 1 9.52
CHEMBL203393 1 9.10
CHEMBL203230 1 8.80
CHEMBL191054 1 8.72
CHEMBL206394 1 8.64
CHEMBL206845 1 8.57
CHEMBL203013 1 8.44
CHEMBL206333 1 7.85
CHEMBL383051 1 7.80
CHEMBL383694 1 7.68
CHEMBL382618 1 7.41
CHEMBL203396 1 7.28
CHEMBL206386 1 7.27
CHEMBL202795 1 7.22
CHEMBL206618 1 7.03
CHEMBL205671 1 6.98
CHEMBL203025 1 6.88
CHEMBL382471 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190699 Ki = 0.3 nM 9.52
CHEMBL203393 Ki = 0.8 nM 9.10
CHEMBL203230 Ki = 1.6 nM 8.80
CHEMBL191054 Ki = 1.9 nM 8.72
CHEMBL206394 Ki = 2.3 nM 8.64
CHEMBL206845 Ki = 2.7 nM 8.57
CHEMBL203013 Ki = 3.6 nM 8.44
CHEMBL206333 Ki = 14.0 nM 7.85
CHEMBL383051 Ki = 16.0 nM 7.80
CHEMBL383694 Ki = 21.0 nM 7.68
CHEMBL382618 Ki = 39.0 nM 7.41
CHEMBL203396 Ki = 52.0 nM 7.28
CHEMBL206386 Ki = 54.0 nM 7.27
CHEMBL202795 Ki = 60.0 nM 7.22
CHEMBL206618 Ki = 93.0 nM 7.03
CHEMBL205671 Ki = 104.0 nM 6.98
CHEMBL203025 Ki = 131.0 nM 6.88
CHEMBL382471 Ki - -