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Assay Detail

CHEMBL913685

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Binding
Binding affinity to dopamine D2
63
Total Activities
63
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(2) dopamine receptor (CHEMBL217)
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 63 6.73 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.95
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.74
CHEMBL217981 1 8.31
CHEMBL221129 1 8.28
CHEMBL221866 1 8.04
CHEMBL221587 1 8.03
CHEMBL221897 1 8.00
CHEMBL425285 1 7.85
CHEMBL220754 1 7.77
CHEMBL386986 1 7.66
CHEMBL139600 1 7.52
CHEMBL221600 1 7.42
CHEMBL373873 1 7.41
CHEMBL210404 1 7.40
CHEMBL218351 1 7.37
CHEMBL437525 1 7.26
CHEMBL218607 1 7.24
CHEMBL385289 1 7.21
CHEMBL210717 1 7.20
CHEMBL218318 1 7.17
CHEMBL140968 1 7.15
CHEMBL208018 1 7.15
CHEMBL424294 1 7.06
CHEMBL221681 1 7.02
CHEMBL218444 1 6.96
CHEMBL124444 1 6.96
CHEMBL376020 1 6.89
CHEMBL374749 1 6.89
CHEMBL210405 1 6.85
CHEMBL220700 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 1.122 nM 8.95
CHEMBL1112 ARIPIPRAZOLE Ki = 1.82 nM 8.74
CHEMBL217981 Ki = 4.898 nM 8.31
CHEMBL221129 Ki = 5.248 nM 8.28
CHEMBL221866 Ki = 9.12 nM 8.04
CHEMBL221587 Ki = 9.333 nM 8.03
CHEMBL221897 Ki = 10.0 nM 8.00
CHEMBL425285 Ki = 14.13 nM 7.85
CHEMBL220754 Ki = 16.98 nM 7.77
CHEMBL386986 Ki = 21.88 nM 7.66
CHEMBL139600 Ki = 30.2 nM 7.52
CHEMBL221600 Ki = 38.02 nM 7.42
CHEMBL373873 Ki = 38.9 nM 7.41
CHEMBL210404 Ki = 39.81 nM 7.40
CHEMBL218351 Ki = 42.66 nM 7.37
CHEMBL437525 Ki = 54.95 nM 7.26
CHEMBL218607 Ki = 57.54 nM 7.24
CHEMBL385289 Ki = 61.66 nM 7.21
CHEMBL210717 Ki = 63.1 nM 7.20
CHEMBL218318 Ki = 67.61 nM 7.17
CHEMBL140968 Ki = 70.79 nM 7.15
CHEMBL208018 Ki = 70.79 nM 7.15
CHEMBL424294 Ki = 87.1 nM 7.06
CHEMBL221681 Ki = 95.5 nM 7.02
CHEMBL124444 Ki = 109.65 nM 6.96
CHEMBL218444 Ki = 109.65 nM 6.96
CHEMBL376020 Ki = 128.82 nM 6.89
CHEMBL374749 Ki = 128.82 nM 6.89
CHEMBL210405 Ki = 141.25 nM 6.85
CHEMBL220700 Ki = 141.25 nM 6.85
CHEMBL344677 Ki = 151.36 nM 6.82
CHEMBL218638 Ki = 158.49 nM 6.80
CHEMBL342060 Ki = 190.55 nM 6.72
CHEMBL218368 Ki = 199.53 nM 6.70
CHEMBL25236 BP-897 Ki = 208.93 nM 6.68
CHEMBL221814 Ki = 218.78 nM 6.66
CHEMBL221843 Ki = 229.09 nM 6.64
CHEMBL143352 Ki = 269.15 nM 6.57
CHEMBL221549 Ki = 281.84 nM 6.55
CHEMBL141845 Ki = 288.4 nM 6.54
CHEMBL142020 Ki = 309.03 nM 6.51
CHEMBL139926 Ki = 323.59 nM 6.49
CHEMBL218151 Ki = 338.84 nM 6.47
CHEMBL425057 Ki = 338.84 nM 6.47
CHEMBL221397 Ki = 407.38 nM 6.39
CHEMBL437490 Ki = 446.68 nM 6.35
CHEMBL218203 Ki = 457.09 nM 6.34
CHEMBL219274 Ki = 467.74 nM 6.33
CHEMBL139722 Ki = 524.81 nM 6.28
CHEMBL377200 Ki = 630.96 nM 6.20