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Assay Detail

CHEMBL3366161

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

Binding
Displacement of [3H]Mesulergine from rat 5-HT2C receptor by liquid scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Further evaluation of the tropane analogs of haloperidol.
Sampson D, Bricker B, Zhu XY, Peprah K, Lamango NS, Setola V, Roth BL, Ablordeppey SY.
Bioorg Med Chem Lett (2014) 24 : 4294 -4297
PubMed 25070422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.75 6.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210578 1 6.06
CHEMBL3321792 1 5.95
CHEMBL3321790 1 5.82
CHEMBL3321791 1 5.73
CHEMBL3321788 1 5.61
CHEMBL54 HALOPERIDOL 4.0 1 5.33
CHEMBL1940404 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210578 Ki = 872.0 nM 6.06
CHEMBL3321792 Ki = 1122.0 nM 5.95
CHEMBL3321790 Ki = 1498.0 nM 5.82
CHEMBL3321791 Ki = 1861.0 nM 5.73
CHEMBL3321788 Ki = 2434.0 nM 5.61
CHEMBL54 HALOPERIDOL Ki = 4700.0 nM 5.33
CHEMBL1940404 Ki > 10000.0 nM -