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Assay Detail

CHEMBL912015

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

Binding
Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane
ChEMBL ↗
66
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(3) dopamine receptor (CHEMBL234) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-selectivity investigations of D2-like receptor ligands by CoMFA and CoMSIA guiding the discovery of D3 selective PET radioligands.
Salama I, Hocke C, Utz W, Prante O, Boeckler F, Hübner H, Kuwert T, Gmeiner P.
J Med Chem (2007) 50 : 489 -500
PubMed 17266201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 66 7.83 9.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424294 — — 1 9.63
CHEMBL218444 — — 1 9.61
CHEMBL218638 — — 1 9.60
CHEMBL374749 — — 2 9.55
CHEMBL218151 — — 1 9.45
CHEMBL221652 — — 1 9.43
CHEMBL218368 — — 1 9.42
CHEMBL221397 — — 1 9.41
CHEMBL221640 — — 1 9.35
CHEMBL218318 — — 1 9.34
CHEMBL59725 — — 1 9.30
CHEMBL220700 — — 1 9.24
CHEMBL346692 — — 1 9.18
CHEMBL221681 — — 1 9.16
CHEMBL218150 — — 1 9.13
CHEMBL218203 — — 1 9.00
CHEMBL139926 — — 1 8.95
CHEMBL124444 — — 1 8.95
CHEMBL25236 BP-897 — 1 8.85
CHEMBL219274 — — 1 8.77
CHEMBL425285 — — 1 8.62
CHEMBL342060 — — 1 8.55
CHEMBL221549 — — 1 8.51
CHEMBL376445 — — 1 8.46
CHEMBL386986 — — 1 8.46
CHEMBL373873 — — 1 8.37
CHEMBL376020 — — 1 8.37
CHEMBL142020 — — 1 8.37
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.35
CHEMBL221129 — — 1 8.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424294 — Ki = 0.2344 nM 9.63
CHEMBL218444 — Ki = 0.2455 nM 9.61
CHEMBL218638 — Ki = 0.2512 nM 9.60
CHEMBL374749 — Ki = 0.28 nM 9.55
CHEMBL374749 — Ki = 0.2818 nM 9.55
CHEMBL218151 — Ki = 0.3548 nM 9.45
CHEMBL221652 — Ki = 0.37 nM 9.43
CHEMBL218368 — Ki = 0.3802 nM 9.42
CHEMBL221397 — Ki = 0.389 nM 9.41
CHEMBL221640 — Ki = 0.45 nM 9.35
CHEMBL218318 — Ki = 0.4571 nM 9.34
CHEMBL59725 — Ki = 0.5012 nM 9.30
CHEMBL220700 — Ki = 0.5754 nM 9.24
CHEMBL346692 — Ki = 0.6607 nM 9.18
CHEMBL221681 — Ki = 0.6918 nM 9.16
CHEMBL218150 — Ki = 0.7413 nM 9.13
CHEMBL218203 — Ki = 1.0 nM 9.00
CHEMBL139926 — Ki = 1.122 nM 8.95
CHEMBL124444 — Ki = 1.122 nM 8.95
CHEMBL25236 BP-897 Ki = 1.413 nM 8.85
CHEMBL219274 — Ki = 1.698 nM 8.77
CHEMBL425285 — Ki = 2.399 nM 8.62
CHEMBL342060 — Ki = 2.818 nM 8.55
CHEMBL221549 — Ki = 3.09 nM 8.51
CHEMBL386986 — Ki = 3.467 nM 8.46
CHEMBL376445 — Ki = 3.467 nM 8.46
CHEMBL376020 — Ki = 4.266 nM 8.37
CHEMBL373873 — Ki = 4.266 nM 8.37
CHEMBL142020 — Ki = 4.266 nM 8.37
CHEMBL1112 ARIPIPRAZOLE Ki = 4.467 nM 8.35
CHEMBL221129 — Ki = 7.413 nM 8.13
CHEMBL54 HALOPERIDOL Ki = 8.318 nM 8.08
CHEMBL221897 — Ki = 8.511 nM 8.07
CHEMBL218607 — Ki = 10.96 nM 7.96
CHEMBL218351 — Ki = 12.88 nM 7.89
CHEMBL217981 — Ki = 15.14 nM 7.82
CHEMBL221587 — Ki = 15.85 nM 7.80
CHEMBL143352 — Ki = 19.95 nM 7.70
CHEMBL437525 — Ki = 28.84 nM 7.54
CHEMBL344677 — Ki = 28.84 nM 7.54
CHEMBL385289 — Ki = 32.36 nM 7.49
CHEMBL221600 — Ki = 33.11 nM 7.48
CHEMBL221866 — Ki = 33.88 nM 7.47
CHEMBL140968 — Ki = 51.29 nM 7.29
CHEMBL139600 — Ki = 64.57 nM 7.19
CHEMBL210717 — Ki = 67.61 nM 7.17
CHEMBL221843 — Ki = 67.61 nM 7.17
CHEMBL210404 — Ki = 72.44 nM 7.14
CHEMBL220754 — Ki = 87.1 nM 7.06
CHEMBL221814 — Ki = 93.33 nM 7.03