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Assay Detail

CHEMBL3801702

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

Binding
Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain cortex incubated for 15 mins
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

5-HT2 receptor affinity, docking studies and pharmacological evaluation of a series of 1,3-disubstituted thiourea derivatives.
Bielenica A, Kędzierska E, Koliński M, Kmiecik S, Koliński A, Fiorino F, Severino B, Magli E, Corvino A, Rossi I, Massarelli P, Kozioł AE, Sawczenko A, Struga M.
Eur J Med Chem (2016) 116 : 173 -186
PubMed 27061981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 9.55 10.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3617113 1 10.37
CHEMBL1404528 1 9.22
CHEMBL51 KETANSERIN 3.0 1 9.07
CHEMBL3797474 1 -
CHEMBL3798961 1 -
CHEMBL3617211 1 -
CHEMBL3798863 1 -
CHEMBL3798450 1 -
CHEMBL3799209 1 -
CHEMBL3797981 1 -
CHEMBL3799165 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3617113 Ki = 0.043 nM 10.37
CHEMBL1404528 Ki = 0.6 nM 9.22
CHEMBL51 KETANSERIN Ki = 0.85 nM 9.07
CHEMBL3797474 Ki > 10000.0 nM -
CHEMBL3798961 Ki > 10000.0 nM -
CHEMBL3617211 Ki > 10000.0 nM -
CHEMBL3798863 Ki > 10000.0 nM -
CHEMBL3798450 Ki > 10000.0 nM -
CHEMBL3799209 Ki > 10000.0 nM -
CHEMBL3797981 Ki > 10000.0 nM -
CHEMBL3799165 Ki > 10000.0 nM -