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Assay Detail

CHEMBL4010153

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

Binding
Displacement of [3H]spiperone from human Dopamine D2S receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of G Protein-Biased Dopaminergics with a Pyrazolo[1,5-a]pyridine Substructure.
Möller D, Banerjee A, Uzuneser TC, Skultety M, Huth T, Plouffe B, Hübner H, Alzheimer C, Friedland K, Müller CP, Bouvier M, Gmeiner P.
J Med Chem (2017) 60 : 2908 -2929
PubMed 28248104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 8.74 10.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4060461 2 10.03
CHEMBL4063235 1 9.80
CHEMBL4060403 1 9.39
CHEMBL1112 ARIPIPRAZOLE 4.0 1 9.35
CHEMBL4069091 1 9.30
CHEMBL4096353 1 9.28
CHEMBL4091064 1 9.28
CHEMBL4070091 1 9.26
CHEMBL4078348 1 9.15
CHEMBL4098803 1 9.13
CHEMBL4097330 1 9.12
CHEMBL4071868 1 9.08
CHEMBL4098859 1 9.06
CHEMBL4090208 1 9.05
CHEMBL4071185 1 9.03
CHEMBL4088639 1 8.82
CHEMBL4069145 1 8.77
CHEMBL4105030 1 8.72
CHEMBL4098236 1 8.64
CHEMBL4087187 1 8.26
CHEMBL4099711 1 8.24
CHEMBL4072821 1 8.13
CHEMBL4067439 1 8.11
CHEMBL4091155 1 8.11
CHEMBL4079301 1 7.92
CHEMBL4080762 1 7.85
CHEMBL4063282 1 7.44
CHEMBL4094869 1 7.41
CHEMBL4102616 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4060461 Ki = 0.094 nM 10.03
CHEMBL4063235 Ki = 0.16 nM 9.80
CHEMBL4060403 Ki = 0.41 nM 9.39
CHEMBL1112 ARIPIPRAZOLE Ki = 0.45 nM 9.35
CHEMBL4069091 Ki = 0.5 nM 9.30
CHEMBL4096353 Ki = 0.52 nM 9.28
CHEMBL4091064 Ki = 0.52 nM 9.28
CHEMBL4070091 Ki = 0.55 nM 9.26
CHEMBL4078348 Ki = 0.7 nM 9.15
CHEMBL4060461 Ki = 0.72 nM 9.14
CHEMBL4098803 Ki = 0.74 nM 9.13
CHEMBL4097330 Ki = 0.75 nM 9.12
CHEMBL4071868 Ki = 0.84 nM 9.08
CHEMBL4098859 Ki = 0.87 nM 9.06
CHEMBL4090208 Ki = 0.9 nM 9.05
CHEMBL4071185 Ki = 0.94 nM 9.03
CHEMBL4088639 Ki = 1.5 nM 8.82
CHEMBL4069145 Ki = 1.7 nM 8.77
CHEMBL4105030 Ki = 1.9 nM 8.72
CHEMBL4098236 Ki = 2.3 nM 8.64
CHEMBL4087187 Ki = 5.5 nM 8.26
CHEMBL4099711 Ki = 5.8 nM 8.24
CHEMBL4072821 Ki = 7.4 nM 8.13
CHEMBL4091155 Ki = 7.8 nM 8.11
CHEMBL4067439 Ki = 7.7 nM 8.11
CHEMBL4079301 Ki = 12.0 nM 7.92
CHEMBL4080762 Ki = 14.0 nM 7.85
CHEMBL4063282 Ki = 36.0 nM 7.44
CHEMBL4094869 Ki = 39.0 nM 7.41
CHEMBL4102616 Ki = 48.0 nM 7.32