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Assay Detail

CHEMBL1069954

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

Binding
Displacement of [125I]DOI from rat 5HT2A receptor expressed in mouse 3T3 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity.
Liu KK, Cornelius P, Patterson TA, Zeng Y, Santucci S, Tomlinson E, Gibbons C, Maurer TS, Marala R, Brown J, Kong JX, Lee E, Werner W, Wenzel Z, Vage C.
Bioorg Med Chem Lett (2010) 20 : 266 -271
PubMed 19914063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.26 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595194 1 9.15
CHEMBL609306 1 9.00
CHEMBL593545 1 8.70
CHEMBL595195 1 8.42
CHEMBL594717 1 8.36
CHEMBL594469 1 7.82
CHEMBL595645 1 7.80
CHEMBL593547 1 7.68
CHEMBL595553 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595194 Ki = 0.7 nM 9.15
CHEMBL609306 Ki = 1.0 nM 9.00
CHEMBL593545 Ki = 2.0 nM 8.70
CHEMBL595195 Ki = 3.8 nM 8.42
CHEMBL594717 Ki = 4.4 nM 8.36
CHEMBL594469 Ki = 15.0 nM 7.82
CHEMBL595645 Ki = 16.0 nM 7.80
CHEMBL593547 Ki = 21.0 nM 7.68
CHEMBL595553 Ki = 41.0 nM 7.39