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Assay Detail

CHEMBL913682

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

Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
65
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(4) dopamine receptor (CHEMBL219)
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 65 7.49 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210404 1 9.36
CHEMBL221600 1 9.23
CHEMBL267014 L-745870 1 9.21
CHEMBL141845 1 9.17
CHEMBL210717 1 9.15
CHEMBL210405 1 9.00
CHEMBL208018 1 9.00
CHEMBL160952 1 8.91
CHEMBL310843 1 8.66
CHEMBL7927 FAUC 113 1 8.64
CHEMBL425057 1 8.59
CHEMBL423247 1 8.57
CHEMBL210955 1 8.54
CHEMBL437490 1 8.54
CHEMBL221814 1 8.49
CHEMBL218787 1 8.30
CHEMBL377200 1 8.28
CHEMBL54 HALOPERIDOL 4.0 1 8.22
CHEMBL344677 1 8.05
CHEMBL424294 1 7.82
CHEMBL218444 1 7.80
CHEMBL221681 1 7.77
CHEMBL345357 1 7.71
CHEMBL220700 1 7.62
CHEMBL221652 1 7.55
CHEMBL139722 1 7.52
CHEMBL124444 1 7.52
CHEMBL221397 1 7.51
CHEMBL221640 1 7.47
CHEMBL25236 BP-897 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210404 Ki = 0.4365 nM 9.36
CHEMBL221600 Ki = 0.5888 nM 9.23
CHEMBL267014 L-745870 Ki = 0.6166 nM 9.21
CHEMBL141845 Ki = 0.6761 nM 9.17
CHEMBL210717 Ki = 0.7079 nM 9.15
CHEMBL210405 Ki = 1.0 nM 9.00
CHEMBL208018 Ki = 1.0 nM 9.00
CHEMBL160952 Ki = 1.23 nM 8.91
CHEMBL310843 Ki = 2.188 nM 8.66
CHEMBL7927 FAUC 113 Ki = 2.291 nM 8.64
CHEMBL425057 Ki = 2.57 nM 8.59
CHEMBL423247 Ki = 2.692 nM 8.57
CHEMBL210955 Ki = 2.884 nM 8.54
CHEMBL437490 Ki = 2.884 nM 8.54
CHEMBL221814 Ki = 3.236 nM 8.49
CHEMBL218787 Ki = 5.012 nM 8.30
CHEMBL377200 Ki = 5.248 nM 8.28
CHEMBL54 HALOPERIDOL Ki = 6.026 nM 8.22
CHEMBL344677 Ki = 8.913 nM 8.05
CHEMBL424294 Ki = 15.14 nM 7.82
CHEMBL218444 Ki = 15.85 nM 7.80
CHEMBL221681 Ki = 16.98 nM 7.77
CHEMBL345357 Ki = 19.5 nM 7.71
CHEMBL220700 Ki = 23.99 nM 7.62
CHEMBL221652 Ki = 28.0 nM 7.55
CHEMBL139722 Ki = 30.2 nM 7.52
CHEMBL124444 Ki = 30.2 nM 7.52
CHEMBL221397 Ki = 30.9 nM 7.51
CHEMBL221640 Ki = 34.0 nM 7.47
CHEMBL25236 BP-897 Ki = 38.9 nM 7.41
CHEMBL221129 Ki = 39.81 nM 7.40
CHEMBL218638 Ki = 39.81 nM 7.40
CHEMBL357684 Ki = 40.74 nM 7.39
CHEMBL217981 Ki = 41.69 nM 7.38
CHEMBL218318 Ki = 44.67 nM 7.35
CHEMBL1112 ARIPIPRAZOLE Ki = 57.54 nM 7.24
CHEMBL376020 Ki = 57.54 nM 7.24
CHEMBL139600 Ki = 67.61 nM 7.17
CHEMBL342060 Ki = 67.61 nM 7.17
CHEMBL386986 Ki = 75.86 nM 7.12
CHEMBL140968 Ki = 77.62 nM 7.11
CHEMBL143352 Ki = 87.1 nM 7.06
CHEMBL385289 Ki = 91.2 nM 7.04
CHEMBL139926 Ki = 93.33 nM 7.03
CHEMBL142020 Ki = 128.82 nM 6.89
CHEMBL218351 Ki = 128.82 nM 6.89
CHEMBL218368 Ki = 151.36 nM 6.82
CHEMBL221587 Ki = 158.49 nM 6.80
CHEMBL221549 Ki = 169.82 nM 6.77
CHEMBL218203 Ki = 199.53 nM 6.70