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Assay Detail

CHEMBL617951

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

Functional
Negative log concentration of antagonist on 5-hydroxytryptamine 2A receptor in rat thoracic aorta
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Thoracic aorta
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
Kd 37 7.62 9.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110948 1 9.87
CHEMBL333174 1 9.50
CHEMBL164471 1 9.25
CHEMBL120903 1 9.20
CHEMBL42 CLOZAPINE 4.0 1 9.16
CHEMBL320572 1 9.13
CHEMBL109673 1 9.02
CHEMBL159969 1 8.92
CHEMBL51 KETANSERIN 3.0 1 8.87
CHEMBL109548 1 8.13
CHEMBL87458 1 8.12
CHEMBL87717 1 8.12
CHEMBL143027 1 7.95
CHEMBL308480 1 7.86
CHEMBL111393 1 7.82
CHEMBL325253 1 7.79
CHEMBL95112 1 7.63
CHEMBL159929 1 7.58
CHEMBL87943 1 7.47
CHEMBL96781 1 7.35
CHEMBL95098 1 7.30
CHEMBL143022 1 7.28
CHEMBL310734 1 7.27
CHEMBL111509 1 7.20
CHEMBL110847 1 6.95
CHEMBL111189 1 6.83
CHEMBL161423 1 6.80
CHEMBL87026 1 6.75
CHEMBL92145 1 6.72
CHEMBL121744 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110948 Kd = 0.1349 nM 9.87
CHEMBL333174 Kd = 0.3162 nM 9.50
CHEMBL164471 Kd = 0.5623 nM 9.25
CHEMBL120903 Kd = 0.631 nM 9.20
CHEMBL42 CLOZAPINE Kd = 0.6918 nM 9.16
CHEMBL320572 Kd = 0.7413 nM 9.13
CHEMBL109673 Kd = 0.955 nM 9.02
CHEMBL159969 Kd = 1.202 nM 8.92
CHEMBL51 KETANSERIN Kd = 1.349 nM 8.87
CHEMBL109548 Kd = 7.413 nM 8.13
CHEMBL87458 Kd = 7.586 nM 8.12
CHEMBL87717 Kd = 7.586 nM 8.12
CHEMBL143027 Kd = 11.22 nM 7.95
CHEMBL308480 Kd = 13.8 nM 7.86
CHEMBL111393 Kd = 15.14 nM 7.82
CHEMBL325253 Kd = 16.22 nM 7.79
CHEMBL95112 Kd = 23.44 nM 7.63
CHEMBL159929 Kd = 26.3 nM 7.58
CHEMBL87943 Kd = 33.88 nM 7.47
CHEMBL96781 Kd = 44.67 nM 7.35
CHEMBL95098 Kd = 50.12 nM 7.30
CHEMBL143022 Kd = 52.48 nM 7.28
CHEMBL310734 Kd = 53.7 nM 7.27
CHEMBL111509 Kd = 63.1 nM 7.20
CHEMBL110847 Kd = 112.2 nM 6.95
CHEMBL111189 Kd = 147.91 nM 6.83
CHEMBL161423 Kd = 158.49 nM 6.80
CHEMBL87026 Kd = 177.83 nM 6.75
CHEMBL92145 Kd = 190.55 nM 6.72
CHEMBL121744 Kd = 316.23 nM 6.50
CHEMBL310153 Kd = 331.13 nM 6.48
CHEMBL159466 Kd = 398.11 nM 6.40
CHEMBL163180 Kd = 489.78 nM 6.31
CHEMBL160019 Kd = 501.19 nM 6.30
CHEMBL444269 Kd = 616.6 nM 6.21
CHEMBL159917 Kd = 676.08 nM 6.17
CHEMBL109528 Kd = 1258.93 nM 5.90