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Assay Detail

CHEMBL671730

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

Binding
Binding affinity for human dopamine receptor D2 by displacing [125I]iodosulpiride expressed in CHO cells
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(omega-(4-(2-methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as dopamine D2 and D3 receptor ligands.
Hackling A, Ghosh R, Perachon S, Mann A, Höltje HD, Wermuth CG, Schwartz JC, Sippl W, Sokoloff P, Stark H.
J Med Chem (2003) 46 : 3883 -3899
PubMed 12930150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 75 7.39 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279247 1 8.21
CHEMBL129035 1 8.14
CHEMBL125459 1 8.10
CHEMBL338552 1 8.02
CHEMBL341241 1 8.00
CHEMBL127038 1 7.99
CHEMBL341299 1 7.96
CHEMBL339062 1 7.94
CHEMBL127311 1 7.92
CHEMBL126280 1 7.89
CHEMBL126128 1 7.87
CHEMBL129465 1 7.85
CHEMBL126441 1 7.85
CHEMBL341542 1 7.84
CHEMBL127654 1 7.82
CHEMBL126136 1 7.82
CHEMBL126474 1 7.76
CHEMBL127234 1 7.75
CHEMBL126834 1 7.75
CHEMBL129767 1 7.72
CHEMBL126258 1 7.71
CHEMBL127912 1 7.70
CHEMBL338063 1 7.68
CHEMBL338606 1 7.68
CHEMBL126892 1 7.68
CHEMBL126725 1 7.65
CHEMBL421085 1 7.64
CHEMBL126780 1 7.64
CHEMBL341134 1 7.62
CHEMBL99198 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279247 Ki = 6.1 nM 8.21
CHEMBL129035 Ki = 7.2 nM 8.14
CHEMBL125459 Ki = 8.0 nM 8.10
CHEMBL338552 Ki = 9.5 nM 8.02
CHEMBL341241 Ki = 10.0 nM 8.00
CHEMBL127038 Ki = 10.3 nM 7.99
CHEMBL341299 Ki = 11.1 nM 7.96
CHEMBL339062 Ki = 11.5 nM 7.94
CHEMBL127311 Ki = 12.0 nM 7.92
CHEMBL126280 Ki = 13.0 nM 7.89
CHEMBL126128 Ki = 13.54 nM 7.87
CHEMBL129465 Ki = 14.0 nM 7.85
CHEMBL126441 Ki = 14.0 nM 7.85
CHEMBL341542 Ki = 14.5 nM 7.84
CHEMBL126136 Ki = 15.2 nM 7.82
CHEMBL127654 Ki = 15.0 nM 7.82
CHEMBL126474 Ki = 17.5 nM 7.76
CHEMBL127234 Ki = 18.0 nM 7.75
CHEMBL126834 Ki = 18.0 nM 7.75
CHEMBL129767 Ki = 19.0 nM 7.72
CHEMBL126258 Ki = 19.5 nM 7.71
CHEMBL127912 Ki = 20.0 nM 7.70
CHEMBL338063 Ki = 21.0 nM 7.68
CHEMBL338606 Ki = 20.7 nM 7.68
CHEMBL126892 Ki = 20.9 nM 7.68
CHEMBL126725 Ki = 22.6 nM 7.65
CHEMBL126780 Ki = 23.0 nM 7.64
CHEMBL421085 Ki = 23.0 nM 7.64
CHEMBL341134 Ki = 23.7 nM 7.62
CHEMBL99198 Ki = 25.0 nM 7.60
CHEMBL127288 Ki = 26.5 nM 7.58
CHEMBL129022 Ki = 27.5 nM 7.56
CHEMBL126312 Ki = 28.4 nM 7.55
CHEMBL340851 Ki = 32.0 nM 7.50
CHEMBL126749 Ki = 32.0 nM 7.50
CHEMBL339103 Ki = 35.0 nM 7.46
CHEMBL126746 Ki = 37.0 nM 7.43
CHEMBL129429 Ki = 36.79 nM 7.43
CHEMBL127923 Ki = 38.5 nM 7.42
CHEMBL126285 Ki = 40.0 nM 7.40
CHEMBL126656 Ki = 44.0 nM 7.36
CHEMBL127807 Ki = 45.0 nM 7.35
CHEMBL125525 Ki = 47.0 nM 7.33
CHEMBL340173 Ki = 48.7 nM 7.31
CHEMBL126632 Ki = 50.0 nM 7.30
CHEMBL415520 Ki = 50.2 nM 7.30
CHEMBL126439 Ki = 53.2 nM 7.27
CHEMBL128133 Ki = 56.0 nM 7.25
CHEMBL127080 Ki = 56.0 nM 7.25
CHEMBL25236 BP-897 Ki = 61.0 nM 7.21