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Assay Detail

CHEMBL872882

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

Binding
Binding affinity towards human Dopamine receptor D2 was determined via standard competitive displacement assay using [3H]-YM 09151 as radioligand
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.
Zhao H, Thurkauf A, He X, Hodgetts K, Zhang X, Rachwal S, Kover RX, Hutchison A, Peterson J, Kieltyka A, Brodbeck R, Primus R, Wasley JW.
Bioorg Med Chem Lett (2002) 12 : 3105 -3109
PubMed 12372512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.01 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104160 1 7.46
CHEMBL317879 1 6.93
CHEMBL326670 1 6.92
CHEMBL326250 1 6.89
CHEMBL319927 1 6.74
CHEMBL441274 1 6.73
CHEMBL106916 1 6.68
CHEMBL106742 1 6.51
CHEMBL104713 1 6.47
CHEMBL323213 1 6.42
CHEMBL105625 1 6.35
CHEMBL319650 1 6.31
CHEMBL107793 1 6.29
CHEMBL69584 1 6.16
CHEMBL107384 1 6.05
CHEMBL106998 1 5.77
CHEMBL107338 1 5.71
CHEMBL106598 1 5.67
CHEMBL107391 1 5.65
CHEMBL321871 1 5.60
CHEMBL317266 1 5.59
CHEMBL323537 1 5.58
CHEMBL104196 1 5.58
CHEMBL107962 1 5.48
CHEMBL321058 1 5.46
CHEMBL106917 1 5.42
CHEMBL318760 1 5.42
CHEMBL106897 1 5.38
CHEMBL320067 1 5.36
CHEMBL107229 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104160 Ki = 35.0 nM 7.46
CHEMBL317879 Ki = 117.0 nM 6.93
CHEMBL326670 Ki = 120.0 nM 6.92
CHEMBL326250 Ki = 129.0 nM 6.89
CHEMBL319927 Ki = 183.0 nM 6.74
CHEMBL441274 Ki = 187.0 nM 6.73
CHEMBL106916 Ki = 209.0 nM 6.68
CHEMBL106742 Ki = 306.0 nM 6.51
CHEMBL104713 Ki = 341.0 nM 6.47
CHEMBL323213 Ki = 377.0 nM 6.42
CHEMBL105625 Ki = 450.0 nM 6.35
CHEMBL319650 Ki = 487.0 nM 6.31
CHEMBL107793 Ki = 509.0 nM 6.29
CHEMBL69584 Ki = 690.0 nM 6.16
CHEMBL107384 Ki = 883.0 nM 6.05
CHEMBL106998 Ki = 1692.0 nM 5.77
CHEMBL107338 Ki = 1926.0 nM 5.71
CHEMBL106598 Ki = 2145.0 nM 5.67
CHEMBL107391 Ki = 2220.0 nM 5.65
CHEMBL321871 Ki = 2524.0 nM 5.60
CHEMBL317266 Ki = 2552.0 nM 5.59
CHEMBL323537 Ki = 2629.0 nM 5.58
CHEMBL104196 Ki = 2610.0 nM 5.58
CHEMBL107962 Ki = 3325.0 nM 5.48
CHEMBL321058 Ki = 3431.0 nM 5.46
CHEMBL106917 Ki = 3780.0 nM 5.42
CHEMBL318760 Ki = 3780.0 nM 5.42
CHEMBL106897 Ki = 4126.0 nM 5.38
CHEMBL320067 Ki = 4375.0 nM 5.36
CHEMBL107229 Ki = 4623.0 nM 5.33
CHEMBL107755 Ki = 5847.0 nM 5.23
CHEMBL105595 Ki = 6357.0 nM 5.20
CHEMBL104251 Ki > 1000.0 nM -
CHEMBL104432 Ki > 1000.0 nM -