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Assay Detail

CHEMBL860444

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

Binding
Displacement of [3H]spiperone from human dopamine D2(short) receptor in rat pituitary GH4C1 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
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 12 5.83 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361035 1 7.22
CHEMBL381019 1 7.22
CHEMBL197381 1 6.64
CHEMBL373032 1 6.30
CHEMBL360424 1 6.01
CHEMBL370652 1 5.89
CHEMBL370823 1 5.82
CHEMBL197225 1 5.75
CHEMBL427555 1 5.35
CHEMBL198580 1 4.75
CHEMBL199186 1 4.54
CHEMBL196866 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361035 Ki = 60.0 nM 7.22
CHEMBL381019 Ki = 60.0 nM 7.22
CHEMBL197381 Ki = 230.0 nM 6.64
CHEMBL373032 Ki = 500.0 nM 6.30
CHEMBL360424 Ki = 980.0 nM 6.01
CHEMBL370652 Ki = 1300.0 nM 5.89
CHEMBL370823 Ki = 1500.0 nM 5.82
CHEMBL197225 Ki = 1800.0 nM 5.75
CHEMBL427555 Ki = 4460.0 nM 5.35
CHEMBL198580 Ki = 18000.0 nM 4.75
CHEMBL199186 Ki = 29000.0 nM 4.54
CHEMBL196866 Ki = 38000.0 nM 4.42