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Assay Detail

CHEMBL3871853

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

Binding
Displacement of [125I]DOI from recombinant human 5-HT2C receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2C receptor.
Schrader TO, Kasem M, Ren A, Feichtinger K, Al Doori B, Wei J, Wu C, Dang H, Le M, Gatlin J, Chase K, Dong J, Whelan KT, Sage C, Grottick AJ, Semple G.
Bioorg Med Chem Lett (2016) 26 : 5877 -5882
PubMed 27864071 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.75 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3959570 1 9.50
CHEMBL3947276 1 9.40
CHEMBL3956394 1 9.40
CHEMBL3912721 1 9.20
CHEMBL3919795 1 9.20
CHEMBL3935339 1 9.10
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 8.10
CHEMBL3895972 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3959570 Ki = 0.3162 nM 9.50
CHEMBL3947276 Ki = 0.3981 nM 9.40
CHEMBL3956394 Ki = 0.3981 nM 9.40
CHEMBL3912721 Ki = 0.631 nM 9.20
CHEMBL3919795 Ki = 0.631 nM 9.20
CHEMBL3935339 Ki = 0.7943 nM 9.10
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 7.943 nM 8.10
CHEMBL3895972 Ki = 794.33 nM 6.10