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Assay Detail

CHEMBL828125

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

Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(1-Benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists.
Egle I, Barriault N, Bordeleau M, Drage J, Dube L, Peragine J, Mazzocco L, Arora J, Jarvie K, Tehim A.
Bioorg Med Chem Lett (2004) 14 : 4847 -4850
PubMed 15341937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.14 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361035 1 8.82
CHEMBL426062 1 8.70
CHEMBL187122 1 8.70
CHEMBL364782 1 8.70
CHEMBL185156 1 8.52
CHEMBL187236 1 8.52
CHEMBL360424 1 8.52
CHEMBL187113 1 8.47
CHEMBL360394 1 8.40
CHEMBL366043 1 8.30
CHEMBL184388 1 8.10
CHEMBL187804 1 7.77
CHEMBL182075 1 7.77
CHEMBL183160 1 7.77
CHEMBL366304 1 7.75
CHEMBL424808 1 7.62
CHEMBL186558 1 7.62
CHEMBL184551 1 7.44
CHEMBL427522 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361035 Ki = 1.5 nM 8.82
CHEMBL426062 Ki = 2.0 nM 8.70
CHEMBL187122 Ki = 2.0 nM 8.70
CHEMBL364782 Ki = 2.0 nM 8.70
CHEMBL185156 Ki = 3.0 nM 8.52
CHEMBL187236 Ki = 3.0 nM 8.52
CHEMBL360424 Ki = 3.0 nM 8.52
CHEMBL187113 Ki = 3.4 nM 8.47
CHEMBL360394 Ki = 4.0 nM 8.40
CHEMBL366043 Ki = 5.0 nM 8.30
CHEMBL184388 Ki = 8.0 nM 8.10
CHEMBL187804 Ki = 17.0 nM 7.77
CHEMBL182075 Ki = 17.0 nM 7.77
CHEMBL183160 Ki = 17.0 nM 7.77
CHEMBL366304 Ki = 18.0 nM 7.75
CHEMBL424808 Ki = 24.0 nM 7.62
CHEMBL186558 Ki = 24.0 nM 7.62
CHEMBL184551 Ki = 36.0 nM 7.44
CHEMBL427522 Ki = 70.0 nM 7.16