Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL617268

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

Binding
Inhibitory constant on 5-hydroxytryptamine 2A receptor of Rat frontal cortex
ChEMBL ↗
58
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New serotonin 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo and heterocycloalkanones.
Brea J, Rodrigo J, Carrieri A, Sanz F, Cadavid MI, Enguix MJ, Villazón M, Mengod G, Caro Y, Masaguer CF, Raviña E, Centeno NB, Carotti A, Loza MI.
J Med Chem (2002) 45 : 54 -71
PubMed 11754579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 58 7.47 9.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 9.51
CHEMBL164471 — — 1 8.97
CHEMBL109673 — — 1 8.84
CHEMBL308480 — — 1 8.80
CHEMBL333174 — — 1 8.80
CHEMBL263790 — — 1 8.76
CHEMBL87717 — — 1 8.60
CHEMBL155486 — — 1 8.57
CHEMBL110948 — — 1 8.56
CHEMBL87458 — — 1 8.42
CHEMBL163012 — — 1 8.37
CHEMBL320572 — — 3 8.33
CHEMBL51 KETANSERIN 3.0 1 8.29
CHEMBL111352 — — 1 8.17
CHEMBL159969 — — 1 8.15
CHEMBL42 CLOZAPINE 4.0 1 8.12
CHEMBL87943 — — 1 8.11
CHEMBL162901 — — 1 8.06
CHEMBL120903 — — 1 8.04
CHEMBL143027 — — 1 7.97
CHEMBL321682 — — 1 7.95
CHEMBL87026 — — 1 7.88
CHEMBL310734 — — 1 7.75
CHEMBL159929 — — 1 7.71
CHEMBL141600 — — 1 7.66
CHEMBL109548 — — 1 7.58
CHEMBL92145 — — 1 7.39
CHEMBL95112 — — 1 7.37
CHEMBL111509 — — 1 7.34
CHEMBL143022 — — 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 0.309 nM 9.51
CHEMBL164471 — Ki = 1.072 nM 8.97
CHEMBL109673 — Ki = 1.445 nM 8.84
CHEMBL308480 — Ki = 1.585 nM 8.80
CHEMBL333174 — Ki = 1.585 nM 8.80
CHEMBL263790 — Ki = 1.738 nM 8.76
CHEMBL87717 — Ki = 2.512 nM 8.60
CHEMBL155486 — Ki = 2.692 nM 8.57
CHEMBL110948 — Ki = 2.754 nM 8.56
CHEMBL87458 — Ki = 3.802 nM 8.42
CHEMBL163012 — Ki = 4.266 nM 8.37
CHEMBL320572 — Ki = 4.677 nM 8.33
CHEMBL51 KETANSERIN Ki = 5.129 nM 8.29
CHEMBL111352 — Ki = 6.761 nM 8.17
CHEMBL159969 — Ki = 7.079 nM 8.15
CHEMBL42 CLOZAPINE Ki = 7.586 nM 8.12
CHEMBL87943 — Ki = 7.762 nM 8.11
CHEMBL162901 — Ki = 8.71 nM 8.06
CHEMBL120903 — Ki = 9.12 nM 8.04
CHEMBL143027 — Ki = 10.72 nM 7.97
CHEMBL321682 — Ki = 11.22 nM 7.95
CHEMBL320572 — Ki = 11.48 nM 7.94
CHEMBL320572 — Ki = 11.75 nM 7.93
CHEMBL87026 — Ki = 13.18 nM 7.88
CHEMBL310734 — Ki = 17.78 nM 7.75
CHEMBL159929 — Ki = 19.5 nM 7.71
CHEMBL141600 — Ki = 21.88 nM 7.66
CHEMBL109548 — Ki = 26.3 nM 7.58
CHEMBL92145 — Ki = 40.74 nM 7.39
CHEMBL95112 — Ki = 42.66 nM 7.37
CHEMBL111509 — Ki = 45.71 nM 7.34
CHEMBL143022 — Ki = 51.29 nM 7.29
CHEMBL54 HALOPERIDOL Ki = 52.48 nM 7.28
CHEMBL160907 — Ki = 53.7 nM 7.27
CHEMBL111393 — Ki = 57.54 nM 7.24
CHEMBL96781 — Ki = 72.44 nM 7.14
CHEMBL155006 — Ki = 91.2 nM 7.04
CHEMBL325253 — Ki = 107.15 nM 6.97
CHEMBL95098 — Ki = 123.03 nM 6.91
CHEMBL110847 — Ki = 144.54 nM 6.84
CHEMBL163180 — Ki = 173.78 nM 6.76
CHEMBL160019 — Ki = 190.55 nM 6.72
CHEMBL161423 — Ki = 194.98 nM 6.71
CHEMBL349832 — Ki = 281.84 nM 6.55
CHEMBL111189 — Ki = 288.4 nM 6.54
CHEMBL159917 — Ki = 354.81 nM 6.45
CHEMBL310153 — Ki = 512.86 nM 6.29
CHEMBL121744 — Ki = 630.96 nM 6.20
CHEMBL444269 — Ki = 891.25 nM 6.05
CHEMBL163605 — Ki = 912.01 nM 6.04