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Assay Detail

CHEMBL3820064

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

ADMET
Displacement of [3H]Mesulergine from human recombinant 5HT2C receptor incubated for 1.5 hrs by microbeta scintillation counting method
11
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
Etukala JR, Zhu XY, Eyunni SV, Onyameh EK, Ofori E, Bricker BA, Kang HJ, Huang XP, Roth BL, Ablordeppey SY.
Bioorg Med Chem (2016) 24 : 3671 -3679
PubMed 27364609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 7 - -
Ki 4 5.77 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818124 2 6.21
CHEMBL3819434 2 5.34
CHEMBL3819567 1 -
CHEMBL2037526 1 -
CHEMBL3818935 1 -
CHEMBL3818478 1 -
CHEMBL3819153 1 -
CHEMBL3818805 1 -
CHEMBL3818881 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818124 Ki = 614.0 nM 6.21
CHEMBL3818124 Ki = 616.6 nM 6.21
CHEMBL3819434 Ki = 4570.88 nM 5.34
CHEMBL3819434 Ki = 4623.0 nM 5.33
CHEMBL3819567 Inhibition < 50.0 % -
CHEMBL2037526 Inhibition < 50.0 % -
CHEMBL3818935 Inhibition < 50.0 % -
CHEMBL3818478 Inhibition < 50.0 % -
CHEMBL3819153 Inhibition < 50.0 % -
CHEMBL3818805 Inhibition < 50.0 % -
CHEMBL3818881 Inhibition < 50.0 % -