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Assay Detail

CHEMBL617628

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

Functional
Negative log concentration of antagonist was determined on 5-hydroxytryptamine 2B receptor of Rat stomach fundus
40
Total Activities
40
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Stomach
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2B (CHEMBL323)
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 39 6.62 7.50
pA2 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95098 1 7.50
CHEMBL87026 1 7.40
CHEMBL120903 1 7.22
CHEMBL308480 1 7.20
CHEMBL110847 1 7.19
CHEMBL87943 1 7.15
CHEMBL92145 1 7.13
CHEMBL159969 1 7.06
CHEMBL444269 1 7.04
CHEMBL163180 1 7.01
CHEMBL349832 1 6.90
CHEMBL111393 1 6.88
CHEMBL121744 1 6.80
CHEMBL111189 1 6.80
CHEMBL96781 1 6.80
CHEMBL109528 1 6.78
CHEMBL143022 1 6.71
CHEMBL160019 1 6.68
CHEMBL109548 1 6.66
CHEMBL159929 1 6.63
CHEMBL143027 1 6.61
CHEMBL87717 1 6.43
CHEMBL142668 1 6.36
CHEMBL159771 1 6.35
CHEMBL333174 1 6.35
CHEMBL109673 1 6.35
CHEMBL164471 1 6.30
CHEMBL320572 1 6.24
CHEMBL110948 1 6.23
CHEMBL142316 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95098 Kd = 31.62 nM 7.50
CHEMBL87026 Kd = 39.81 nM 7.40
CHEMBL120903 Kd = 60.26 nM 7.22
CHEMBL308480 Kd = 63.1 nM 7.20
CHEMBL110847 Kd = 64.57 nM 7.19
CHEMBL87943 Kd = 70.79 nM 7.15
CHEMBL92145 Kd = 74.13 nM 7.13
CHEMBL159969 Kd = 87.1 nM 7.06
CHEMBL444269 Kd = 91.2 nM 7.04
CHEMBL163180 Kd = 97.72 nM 7.01
CHEMBL349832 Kd = 125.89 nM 6.90
CHEMBL111393 Kd = 131.83 nM 6.88
CHEMBL121744 Kd = 158.49 nM 6.80
CHEMBL111189 Kd = 158.49 nM 6.80
CHEMBL96781 Kd = 158.49 nM 6.80
CHEMBL109528 Kd = 165.96 nM 6.78
CHEMBL143022 Kd = 194.98 nM 6.71
CHEMBL160019 Kd = 208.93 nM 6.68
CHEMBL109548 Kd = 218.78 nM 6.66
CHEMBL159929 Kd = 234.42 nM 6.63
CHEMBL143027 Kd = 245.47 nM 6.61
CHEMBL87717 Kd = 371.54 nM 6.43
CHEMBL142668 Kd = 436.52 nM 6.36
CHEMBL159771 Kd = 446.68 nM 6.35
CHEMBL333174 Kd = 446.68 nM 6.35
CHEMBL109673 Kd = 446.68 nM 6.35
CHEMBL164471 Kd = 501.19 nM 6.30
CHEMBL320572 Kd = 575.44 nM 6.24
CHEMBL110948 Kd = 588.84 nM 6.23
CHEMBL142316 Kd = 588.84 nM 6.23
CHEMBL87458 Kd = 758.58 nM 6.12
CHEMBL325253 Kd = 2511.89 nM 5.60
CHEMBL159466 Kd = 6606.93 nM 5.18
CHEMBL160907 Kd = 7244.36 nM 5.14
CHEMBL310153 pA2 - -
CHEMBL95112 Kd > 10000.0 nM -
CHEMBL111509 Kd > 10000.0 nM -
CHEMBL310734 Kd > 10000.0 nM -
CHEMBL159917 Kd > 10000.0 nM -
CHEMBL141600 Kd > 10000.0 nM -