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Assay Detail

CHEMBL1069947

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Functional
Agonist activity against human 5HT2C receptor by FLIPR assay relative to 5HT
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

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 22 7.68 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL609306 1 9.15
CHEMBL595195 1 9.05
CHEMBL596327 1 9.00
CHEMBL594717 1 8.82
CHEMBL595194 1 8.82
CHEMBL595646 1 8.40
CHEMBL595645 1 8.15
CHEMBL593545 1 8.00
CHEMBL608135 1 7.85
CHEMBL595553 1 7.70
CHEMBL595555 1 7.66
CHEMBL595196 1 7.64
CHEMBL594469 1 7.60
CHEMBL594718 1 7.55
CHEMBL593547 1 7.35
CHEMBL594477 1 6.95
CHEMBL596108 1 6.90
CHEMBL596328 1 6.81
CHEMBL609595 1 6.68
CHEMBL594489 1 6.42
CHEMBL595866 1 6.35
CHEMBL595554 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL609306 Ki = 0.7 nM 9.15
CHEMBL595195 Ki = 0.9 nM 9.05
CHEMBL596327 Ki = 1.0 nM 9.00
CHEMBL594717 Ki = 1.5 nM 8.82
CHEMBL595194 Ki = 1.5 nM 8.82
CHEMBL595646 Ki = 4.0 nM 8.40
CHEMBL595645 Ki = 7.0 nM 8.15
CHEMBL593545 Ki = 10.0 nM 8.00
CHEMBL608135 Ki = 14.0 nM 7.85
CHEMBL595553 Ki = 20.0 nM 7.70
CHEMBL595555 Ki = 22.0 nM 7.66
CHEMBL595196 Ki = 23.0 nM 7.64
CHEMBL594469 Ki = 25.0 nM 7.60
CHEMBL594718 Ki = 28.0 nM 7.55
CHEMBL593547 Ki = 45.0 nM 7.35
CHEMBL594477 Ki = 113.0 nM 6.95
CHEMBL596108 Ki = 127.0 nM 6.90
CHEMBL596328 Ki = 156.0 nM 6.81
CHEMBL609595 Ki = 207.0 nM 6.68
CHEMBL594489 Ki = 378.0 nM 6.42
CHEMBL595866 Ki = 450.0 nM 6.35
CHEMBL595554 Ki = 755.0 nM 6.12