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Assay Detail

CHEMBL617877

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Binding
Inhibitory constant was determined on 5-hydroxytryptamine 2C receptor of Bovine choroid plexus
ChEMBL ↗
58
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL225) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.46 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.80
CHEMBL162901 — — 1 7.45
CHEMBL85 RISPERIDONE 4.0 1 7.38
CHEMBL51 KETANSERIN 3.0 1 7.36
CHEMBL333174 — — 1 7.24
CHEMBL164471 — — 1 7.16
CHEMBL111352 — — 1 7.16
CHEMBL110847 — — 1 7.09
CHEMBL263790 — — 1 7.06
CHEMBL155486 — — 1 6.98
CHEMBL320572 — — 3 6.95
CHEMBL110948 — — 1 6.90
CHEMBL87717 — — 1 6.78
CHEMBL87943 — — 1 6.65
CHEMBL155006 — — 1 6.65
CHEMBL143937 — — 1 6.64
CHEMBL163605 — — 1 6.63
CHEMBL92145 — — 1 6.63
CHEMBL308480 — — 1 6.63
CHEMBL161423 — — 1 6.55
CHEMBL109673 — — 1 6.48
CHEMBL159929 — — 1 6.46
CHEMBL321682 — — 1 6.45
CHEMBL444269 — — 1 6.44
CHEMBL163012 — — 1 6.42
CHEMBL111189 — — 1 6.40
CHEMBL159969 — — 1 6.38
CHEMBL87026 — — 1 6.30
CHEMBL160019 — — 1 6.24
CHEMBL120903 — — 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 15.85 nM 7.80
CHEMBL162901 — Ki = 35.48 nM 7.45
CHEMBL85 RISPERIDONE Ki = 41.69 nM 7.38
CHEMBL51 KETANSERIN Ki = 43.65 nM 7.36
CHEMBL333174 — Ki = 57.54 nM 7.24
CHEMBL111352 — Ki = 69.18 nM 7.16
CHEMBL164471 — Ki = 69.18 nM 7.16
CHEMBL110847 — Ki = 81.28 nM 7.09
CHEMBL263790 — Ki = 87.1 nM 7.06
CHEMBL155486 — Ki = 104.71 nM 6.98
CHEMBL320572 — Ki = 112.2 nM 6.95
CHEMBL110948 — Ki = 125.89 nM 6.90
CHEMBL320572 — Ki = 144.54 nM 6.84
CHEMBL87717 — Ki = 165.96 nM 6.78
CHEMBL320572 — Ki = 204.17 nM 6.69
CHEMBL155006 — Ki = 223.87 nM 6.65
CHEMBL87943 — Ki = 223.87 nM 6.65
CHEMBL143937 — Ki = 229.09 nM 6.64
CHEMBL92145 — Ki = 234.42 nM 6.63
CHEMBL163605 — Ki = 234.42 nM 6.63
CHEMBL308480 — Ki = 234.42 nM 6.63
CHEMBL161423 — Ki = 281.84 nM 6.55
CHEMBL109673 — Ki = 331.13 nM 6.48
CHEMBL159929 — Ki = 346.74 nM 6.46
CHEMBL321682 — Ki = 354.81 nM 6.45
CHEMBL444269 — Ki = 363.08 nM 6.44
CHEMBL163012 — Ki = 380.19 nM 6.42
CHEMBL111189 — Ki = 398.11 nM 6.40
CHEMBL159969 — Ki = 416.87 nM 6.38
CHEMBL87026 — Ki = 501.19 nM 6.30
CHEMBL160019 — Ki = 575.44 nM 6.24
CHEMBL120903 — Ki = 588.84 nM 6.23
CHEMBL87458 — Ki = 831.76 nM 6.08
CHEMBL159771 — Ki = 851.14 nM 6.07
CHEMBL109528 — Ki = 912.01 nM 6.04
CHEMBL111393 — Ki = 933.25 nM 6.03
CHEMBL109548 — Ki = 1096.48 nM 5.96
CHEMBL121744 — Ki = 1202.26 nM 5.92
CHEMBL163180 — Ki = 1698.24 nM 5.77
CHEMBL160907 — Ki = 1949.84 nM 5.71
CHEMBL310153 — Ki = 2818.38 nM 5.55
CHEMBL96781 — Ki = 3311.31 nM 5.48
CHEMBL349832 — Ki = 3630.78 nM 5.44
CHEMBL325253 — Ki = 3981.07 nM 5.40
CHEMBL54 HALOPERIDOL Ki = 4570.88 nM 5.34
CHEMBL95098 — Ki = 6165.95 nM 5.21
CHEMBL142668 — Ki < 10000.0 nM -
CHEMBL159466 — Ki < 10000.0 nM -
CHEMBL95112 — Ki < 10000.0 nM -
CHEMBL159917 — Ki < 10000.0 nM -