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Assay Detail

CHEMBL1026421

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

Binding
Displacement of [3H]ketanserin from human cloned 5HT2A receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.
Aranda R, Villalba K, Raviña E, Masaguer CF, Brea J, Areias F, Domínguez E, Selent J, López L, Sanz F, Pastor M, Loza MI.
J Med Chem (2008) 51 : 6085 -6094
PubMed 18783204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.81 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164471 1 9.14
CHEMBL461627 1 8.81
CHEMBL492689 1 8.60
CHEMBL523680 1 8.29
CHEMBL143027 1 8.26
CHEMBL516809 1 8.16
CHEMBL459930 1 8.08
CHEMBL42 CLOZAPINE 4.0 1 8.04
CHEMBL494701 1 7.76
CHEMBL494702 1 7.66
CHEMBL493069 1 7.59
CHEMBL159929 1 7.11
CHEMBL143022 1 7.02
CHEMBL54 HALOPERIDOL 4.0 1 6.78
CHEMBL516944 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164471 Ki = 0.7244 nM 9.14
CHEMBL461627 Ki = 1.549 nM 8.81
CHEMBL492689 Ki = 2.512 nM 8.60
CHEMBL523680 Ki = 5.129 nM 8.29
CHEMBL143027 Ki = 5.495 nM 8.26
CHEMBL516809 Ki = 6.918 nM 8.16
CHEMBL459930 Ki = 8.318 nM 8.08
CHEMBL42 CLOZAPINE Ki = 9.12 nM 8.04
CHEMBL494701 Ki = 17.38 nM 7.76
CHEMBL494702 Ki = 21.88 nM 7.66
CHEMBL493069 Ki = 25.7 nM 7.59
CHEMBL159929 Ki = 77.62 nM 7.11
CHEMBL143022 Ki = 95.5 nM 7.02
CHEMBL54 HALOPERIDOL Ki = 165.96 nM 6.78
CHEMBL516944 Ki = 1318.26 nM 5.88