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Assay Detail

CHEMBL854096

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

Binding
Displacement of [3H]5-HT from human 5HT2C
16
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 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.
Adams DR, Bentley JM, Benwell KR, Bickerdike MJ, Bodkin CD, Cliffe IA, Dourish CT, George AR, Kennett GA, Knight AR, Malcolm CS, Mansell HL, Misra A, Quirk K, Roffey JR, Vickers SP.
Bioorg Med Chem Lett (2006) 16 : 677 -680
PubMed 16257207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.64 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201930 1 8.80
CHEMBL76781 1 8.64
CHEMBL201454 1 8.62
CHEMBL39 SEROTONIN 3.0 1 8.16
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 8.05
CHEMBL202458 1 7.80
CHEMBL202616 1 7.80
CHEMBL201062 1 7.57
CHEMBL201897 1 7.43
CHEMBL202538 1 7.41
CHEMBL202656 1 7.14
CHEMBL201117 1 7.11
CHEMBL380763 1 7.11
CHEMBL202324 1 7.07
CHEMBL383042 1 6.78
CHEMBL379223 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201930 Ki = 1.6 nM 8.80
CHEMBL76781 Ki = 2.3 nM 8.64
CHEMBL201454 Ki = 2.4 nM 8.62
CHEMBL39 SEROTONIN Ki = 6.9 nM 8.16
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 9.0 nM 8.05
CHEMBL202458 Ki = 16.0 nM 7.80
CHEMBL202616 Ki = 16.0 nM 7.80
CHEMBL201062 Ki = 27.0 nM 7.57
CHEMBL201897 Ki = 37.0 nM 7.43
CHEMBL202538 Ki = 39.0 nM 7.41
CHEMBL202656 Ki = 72.0 nM 7.14
CHEMBL201117 Ki = 78.0 nM 7.11
CHEMBL380763 Ki = 77.0 nM 7.11
CHEMBL202324 Ki = 86.0 nM 7.07
CHEMBL383042 Ki = 168.0 nM 6.78
CHEMBL379223 Ki = 171.0 nM 6.77