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Assay Detail

CHEMBL860441

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

Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
16
Total Activities
16
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

D(4) dopamine receptor (CHEMBL219)
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 16 7.94 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361035 1 8.82
CHEMBL83894 FANANSERIN 2.0 1 8.54
CHEMBL360424 1 8.52
CHEMBL381019 1 8.40
CHEMBL370823 1 8.30
CHEMBL197225 1 8.15
CHEMBL370134 1 7.85
CHEMBL427555 1 7.85
CHEMBL198580 1 7.85
CHEMBL199186 1 7.82
CHEMBL197381 1 7.80
CHEMBL370652 1 7.68
CHEMBL372770 1 7.66
CHEMBL196866 1 7.48
CHEMBL373032 1 7.28
CHEMBL383383 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361035 Ki = 1.5 nM 8.82
CHEMBL83894 FANANSERIN Ki = 2.9 nM 8.54
CHEMBL360424 Ki = 3.0 nM 8.52
CHEMBL381019 Ki = 4.0 nM 8.40
CHEMBL370823 Ki = 5.0 nM 8.30
CHEMBL197225 Ki = 7.0 nM 8.15
CHEMBL370134 Ki = 14.0 nM 7.85
CHEMBL427555 Ki = 14.0 nM 7.85
CHEMBL198580 Ki = 14.0 nM 7.85
CHEMBL199186 Ki = 15.0 nM 7.82
CHEMBL197381 Ki = 16.0 nM 7.80
CHEMBL370652 Ki = 21.0 nM 7.68
CHEMBL372770 Ki = 22.0 nM 7.66
CHEMBL196866 Ki = 33.0 nM 7.48
CHEMBL373032 Ki = 52.0 nM 7.28
CHEMBL383383 Ki = 78.0 nM 7.11