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Assay Detail

CHEMBL617508

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

Binding
Binding affinity against human 5-hydroxytryptamine 2C receptor using displacement of [3H]DOB
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
Bös M, Jenck F, Martin JR, Moreau JL, Sleight AJ, Wichmann J, Widmer U.
J Med Chem (1997) 40 : 2762 -2769
PubMed 9276022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 8.23 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318639 1 9.40
CHEMBL414163 1 9.00
CHEMBL40726 1 9.00
CHEMBL2114265 1 9.00
CHEMBL76781 1 8.90
CHEMBL2115254 1 8.90
CHEMBL2114266 1 8.90
CHEMBL313856 1 8.70
CHEMBL93154 1 8.50
CHEMBL328761 1 8.50
CHEMBL92656 1 8.40
CHEMBL276673 1 8.40
CHEMBL91855 1 8.40
CHEMBL2115252 1 8.40
CHEMBL320145 1 8.40
CHEMBL3350300 1 8.40
CHEMBL94272 1 8.30
CHEMBL317677 1 8.20
CHEMBL96883 1 8.20
CHEMBL328844 1 8.10
CHEMBL92565 1 8.10
CHEMBL96312 1 8.10
CHEMBL574985 1 8.00
CHEMBL96816 1 8.00
CHEMBL96876 1 7.90
CHEMBL273304 1 7.90
CHEMBL92040 1 7.80
CHEMBL93850 1 7.20
CHEMBL319998 1 7.00
CHEMBL96095 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318639 Ki = 0.3981 nM 9.40
CHEMBL414163 Ki = 1.0 nM 9.00
CHEMBL40726 Ki = 1.0 nM 9.00
CHEMBL2114265 Ki = 1.0 nM 9.00
CHEMBL76781 Ki = 1.259 nM 8.90
CHEMBL2115254 Ki = 1.259 nM 8.90
CHEMBL2114266 Ki = 1.259 nM 8.90
CHEMBL313856 Ki = 1.995 nM 8.70
CHEMBL93154 Ki = 3.162 nM 8.50
CHEMBL328761 Ki = 3.162 nM 8.50
CHEMBL92656 Ki = 3.981 nM 8.40
CHEMBL276673 Ki = 3.981 nM 8.40
CHEMBL91855 Ki = 3.981 nM 8.40
CHEMBL2115252 Ki = 3.981 nM 8.40
CHEMBL320145 Ki = 3.981 nM 8.40
CHEMBL3350300 Ki = 3.981 nM 8.40
CHEMBL94272 Ki = 5.012 nM 8.30
CHEMBL317677 Ki = 6.31 nM 8.20
CHEMBL96883 Ki = 6.31 nM 8.20
CHEMBL96312 Ki = 7.943 nM 8.10
CHEMBL92565 Ki = 7.943 nM 8.10
CHEMBL328844 Ki = 7.943 nM 8.10
CHEMBL574985 Ki = 10.0 nM 8.00
CHEMBL96816 Ki = 10.0 nM 8.00
CHEMBL96876 Ki = 12.59 nM 7.90
CHEMBL273304 Ki = 12.59 nM 7.90
CHEMBL92040 Ki = 15.85 nM 7.80
CHEMBL93850 Ki = 63.1 nM 7.20
CHEMBL319998 Ki = 100.0 nM 7.00
CHEMBL96095 Ki = 125.89 nM 6.90
CHEMBL317564 Ki = 794.33 nM 6.10