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Assay Detail

CHEMBL1040202

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

Binding
Binding affinity to 5-HT2B receptor
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia.
Rotella DP, McFarlane GR, Greenfield A, Grosanu C, Robichaud AJ, Denny RA, Feenstra RW, Núñez-García S, Reinders JH, Neut Mv, McCreary A, Kruse CG, Sullivan K, Pruthi F, Lai M, Zhang J, Kowal DM, Carrick T, Grauer SM, Navarra RL, Graf R, Brennan J, Marquis KL, Pausch MH.
Bioorg Med Chem Lett (2009) 19 : 5552 -5555
PubMed 19720528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.80 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL569251 2 8.22
CHEMBL566396 1 6.96
CHEMBL566356 1 6.78
CHEMBL566379 2 6.40
CHEMBL569513 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL569251 Ki = 6.0 nM 8.22
CHEMBL566396 Ki = 110.0 nM 6.96
CHEMBL569251 Ki = 130.0 nM 6.89
CHEMBL566356 Ki = 165.0 nM 6.78
CHEMBL566379 Ki = 400.0 nM 6.40
CHEMBL566379 Ki = 610.0 nM 6.21
CHEMBL569513 Ki = 680.0 nM 6.17