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Assay Detail

CHEMBL798103

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

Functional
Efficacy (pEC50) was evaluated for 5-HT2C receptor-mediated stimulation of IP3 formation in vitro in choroid plexus of the rat
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Choroid plexus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL324)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
EC50 30 6.01 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318639 1 7.00
CHEMBL2115252 1 6.90
CHEMBL96816 1 6.80
CHEMBL94272 1 6.70
CHEMBL328761 1 6.70
CHEMBL76781 1 6.70
CHEMBL40726 1 6.70
CHEMBL2114265 1 6.60
CHEMBL2114266 1 6.50
CHEMBL414163 1 6.40
CHEMBL313856 1 6.40
CHEMBL96312 1 6.30
CHEMBL93154 1 6.20
CHEMBL92656 1 6.20
CHEMBL2115254 1 6.10
CHEMBL92565 1 5.90
CHEMBL96883 1 5.80
CHEMBL273304 1 5.70
CHEMBL328844 1 5.70
CHEMBL276673 1 5.70
CHEMBL91855 1 5.60
CHEMBL93850 1 5.60
CHEMBL317677 1 5.60
CHEMBL320145 1 5.60
CHEMBL574985 1 5.50
CHEMBL96876 1 5.20
CHEMBL92040 1 5.10
CHEMBL3350300 1 5.10
CHEMBL317564 1 5.00
CHEMBL96095 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318639 EC50 = 100.0 nM 7.00
CHEMBL2115252 EC50 = 125.89 nM 6.90
CHEMBL96816 EC50 = 158.49 nM 6.80
CHEMBL94272 EC50 = 199.53 nM 6.70
CHEMBL328761 EC50 = 199.53 nM 6.70
CHEMBL76781 EC50 = 199.53 nM 6.70
CHEMBL40726 EC50 = 199.53 nM 6.70
CHEMBL2114265 EC50 = 251.19 nM 6.60
CHEMBL2114266 EC50 = 316.23 nM 6.50
CHEMBL414163 EC50 = 398.11 nM 6.40
CHEMBL313856 EC50 = 398.11 nM 6.40
CHEMBL96312 EC50 = 501.19 nM 6.30
CHEMBL93154 EC50 = 630.96 nM 6.20
CHEMBL92656 EC50 = 630.96 nM 6.20
CHEMBL2115254 EC50 = 794.33 nM 6.10
CHEMBL92565 EC50 = 1258.93 nM 5.90
CHEMBL96883 EC50 = 1584.89 nM 5.80
CHEMBL273304 EC50 = 1995.26 nM 5.70
CHEMBL328844 EC50 = 1995.26 nM 5.70
CHEMBL276673 EC50 = 1995.26 nM 5.70
CHEMBL91855 EC50 = 2511.89 nM 5.60
CHEMBL93850 EC50 = 2511.89 nM 5.60
CHEMBL317677 EC50 = 2511.89 nM 5.60
CHEMBL320145 EC50 = 2511.89 nM 5.60
CHEMBL574985 EC50 = 3162.28 nM 5.50
CHEMBL96876 EC50 = 6309.57 nM 5.20
CHEMBL92040 EC50 = 7943.28 nM 5.10
CHEMBL3350300 EC50 = 7943.28 nM 5.10
CHEMBL317564 EC50 = 10000.0 nM 5.00
CHEMBL96095 EC50 = 12589.25 nM 4.90