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Assay Detail

CHEMBL617495

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

Binding
Displacement of [3H]mesulergine from rat 5-HT2C receptor expressed in HEK293
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists.
Forbes IT, Dabbs S, Duckworth DM, Ham P, Jones GE, King FD, Saunders DV, Blaney FE, Naylor CB, Baxter GS, Blackburn TP, Kennett GA, Wood MD.
J Med Chem (1996) 39 : 4966 -4977
PubMed 8960557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.47 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148346 1 8.60
CHEMBL297784 1 8.30
CHEMBL148385 1 8.10
CHEMBL343666 1 8.10
CHEMBL147820 1 8.00
CHEMBL2112859 1 7.90
CHEMBL315223 1 7.60
CHEMBL343455 1 7.40
CHEMBL356146 1 7.30
CHEMBL147368 1 7.20
CHEMBL144567 1 7.20
CHEMBL148347 1 6.90
CHEMBL357870 1 6.90
CHEMBL342776 1 6.70
CHEMBL146830 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148346 Ki = 2.512 nM 8.60
CHEMBL297784 Ki = 5.012 nM 8.30
CHEMBL148385 Ki = 7.943 nM 8.10
CHEMBL343666 Ki = 7.943 nM 8.10
CHEMBL147820 Ki = 10.0 nM 8.00
CHEMBL2112859 Ki = 12.59 nM 7.90
CHEMBL315223 Ki = 25.12 nM 7.60
CHEMBL343455 Ki = 39.81 nM 7.40
CHEMBL356146 Ki = 50.12 nM 7.30
CHEMBL147368 Ki = 63.1 nM 7.20
CHEMBL144567 Ki = 63.1 nM 7.20
CHEMBL148347 Ki = 125.89 nM 6.90
CHEMBL357870 Ki = 125.89 nM 6.90
CHEMBL342776 Ki = 199.53 nM 6.70
CHEMBL146830 Ki = 1258.93 nM 5.90