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Assay Detail

CHEMBL860442

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

Binding
Displacement of [3H]ketanserin from cloned human 5HT2A receptor in HEK298 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK298
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: human dopamine D4 ligands with high affinity for the 5-HT2A receptor.
Arora J, Bordeleau M, Dube L, Jarvie K, Mazzocco L, Peragine J, Tehim A, Egle I.
Bioorg Med Chem Lett (2005) 15 : 5253 -5256
PubMed 16168646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.14 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83894 FANANSERIN 2.0 1 9.43
CHEMBL360424 1 8.74
CHEMBL370823 1 7.85
CHEMBL198580 1 7.80
CHEMBL427555 1 7.66
CHEMBL199186 1 7.66
CHEMBL370134 1 6.89
CHEMBL383383 1 6.85
CHEMBL361035 1 6.34
CHEMBL381019 1 6.21
CHEMBL370652 1 6.13
CHEMBL197381 1 5.96
CHEMBL373032 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83894 FANANSERIN Ki = 0.37 nM 9.43
CHEMBL360424 Ki = 1.8 nM 8.74
CHEMBL370823 Ki = 14.0 nM 7.85
CHEMBL198580 Ki = 16.0 nM 7.80
CHEMBL427555 Ki = 22.0 nM 7.66
CHEMBL199186 Ki = 22.0 nM 7.66
CHEMBL370134 Ki = 130.0 nM 6.89
CHEMBL383383 Ki = 140.0 nM 6.85
CHEMBL361035 Ki = 460.0 nM 6.34
CHEMBL381019 Ki = 610.0 nM 6.21
CHEMBL370652 Ki = 740.0 nM 6.13
CHEMBL197381 Ki = 1100.0 nM 5.96
CHEMBL373032 Ki = 5600.0 nM 5.25