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Assay Detail

CHEMBL892801

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

Binding
Displacement of [3H]ketanserin from serotonin 5HT2A receptor in rat brain cortex
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel class of arylpiperazines containing N-acylated amino acids: their synthesis, 5-HT1A, 5-HT2A receptor affinity, and in vivo pharmacological evaluation.
Zajdel P, Subra G, Bojarski AJ, Duszyńska B, Tatarczyńska E, Nikiforuk A, Chojnacka-Wójcik E, Pawłowski M, Martinez J.
Bioorg Med Chem (2007) 15 : 2907 -2919
PubMed 17321139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.93 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390037 1 8.38
CHEMBL408589 1 8.19
CHEMBL231825 1 7.60
CHEMBL232247 1 7.46
CHEMBL398209 1 7.33
CHEMBL209007 1 7.33
CHEMBL390659 1 7.16
CHEMBL398181 1 6.92
CHEMBL232449 1 6.85
CHEMBL208905 1 6.76
CHEMBL378298 1 6.74
CHEMBL232246 1 6.30
CHEMBL232036 1 6.26
CHEMBL232035 1 6.00
CHEMBL279841 1 5.82
CHEMBL207493 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390037 Ki = 4.2 nM 8.38
CHEMBL408589 Ki = 6.51 nM 8.19
CHEMBL231825 Ki = 25.0 nM 7.60
CHEMBL232247 Ki = 35.0 nM 7.46
CHEMBL398209 Ki = 47.0 nM 7.33
CHEMBL209007 Ki = 47.0 nM 7.33
CHEMBL390659 Ki = 69.0 nM 7.16
CHEMBL398181 Ki = 121.0 nM 6.92
CHEMBL232449 Ki = 140.0 nM 6.85
CHEMBL208905 Ki = 173.0 nM 6.76
CHEMBL378298 Ki = 183.0 nM 6.74
CHEMBL232246 Ki = 503.0 nM 6.30
CHEMBL232036 Ki = 547.0 nM 6.26
CHEMBL232035 Ki = 990.0 nM 6.00
CHEMBL279841 Ki = 1510.0 nM 5.82
CHEMBL207493 Ki = 1510.0 nM 5.82