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Assay Detail

CHEMBL3413541

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

Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D2 receptor expressed in CHOK1 cells incubated for 60 mins by scintillation counting method
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.
Kołaczkowski M, Marcinkowska M, Bucki A, Śniecikowska J, Pawłowski M, Kazek G, Siwek A, Jastrzębska-Więsek M, Partyka A, Wasik A, Wesołowska A, Mierzejewski P, Bienkowski P.
Eur J Med Chem (2015) 92 : 221 -235
PubMed 25557493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.45 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3409242 1 8.89
CHEMBL3409238 1 8.89
CHEMBL54 HALOPERIDOL 4.0 1 8.40
CHEMBL3409234 1 8.32
CHEMBL3409240 1 8.21
CHEMBL3409256 1 8.20
CHEMBL3409239 1 7.96
CHEMBL3409241 1 7.92
CHEMBL3407518 1 7.85
CHEMBL3409237 1 7.70
CHEMBL3409250 1 7.68
CHEMBL3409254 1 7.64
CHEMBL3409245 1 7.54
CHEMBL3409243 1 7.51
CHEMBL3409233 1 7.40
CHEMBL3409252 1 7.36
CHEMBL3409251 1 7.35
CHEMBL3409263 1 7.33
CHEMBL3409246 1 7.21
CHEMBL3409261 1 7.21
CHEMBL3409262 1 7.17
CHEMBL3409235 1 7.16
CHEMBL3409232 1 7.14
CHEMBL3409253 1 7.12
CHEMBL3409257 1 7.11
CHEMBL3409249 1 7.02
CHEMBL3409258 1 6.96
CHEMBL3409236 1 6.92
CHEMBL3409259 1 6.92
CHEMBL3409244 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3409242 Ki = 1.3 nM 8.89
CHEMBL3409238 Ki = 1.3 nM 8.89
CHEMBL54 HALOPERIDOL Ki = 4.0 nM 8.40
CHEMBL3409234 Ki = 4.8 nM 8.32
CHEMBL3409240 Ki = 6.1 nM 8.21
CHEMBL3409256 Ki = 6.3 nM 8.20
CHEMBL3409239 Ki = 11.0 nM 7.96
CHEMBL3409241 Ki = 12.0 nM 7.92
CHEMBL3407518 Ki = 14.0 nM 7.85
CHEMBL3409237 Ki = 20.0 nM 7.70
CHEMBL3409250 Ki = 21.0 nM 7.68
CHEMBL3409254 Ki = 23.0 nM 7.64
CHEMBL3409245 Ki = 29.0 nM 7.54
CHEMBL3409243 Ki = 31.0 nM 7.51
CHEMBL3409233 Ki = 40.0 nM 7.40
CHEMBL3409252 Ki = 44.0 nM 7.36
CHEMBL3409251 Ki = 45.0 nM 7.35
CHEMBL3409263 Ki = 47.0 nM 7.33
CHEMBL3409246 Ki = 62.0 nM 7.21
CHEMBL3409261 Ki = 62.0 nM 7.21
CHEMBL3409262 Ki = 67.0 nM 7.17
CHEMBL3409235 Ki = 70.0 nM 7.16
CHEMBL3409232 Ki = 73.0 nM 7.14
CHEMBL3409253 Ki = 76.0 nM 7.12
CHEMBL3409257 Ki = 78.0 nM 7.11
CHEMBL3409249 Ki = 95.0 nM 7.02
CHEMBL3409258 Ki = 110.0 nM 6.96
CHEMBL3409236 Ki = 120.0 nM 6.92
CHEMBL3409259 Ki = 120.0 nM 6.92
CHEMBL3409244 Ki = 160.0 nM 6.80
CHEMBL3409248 Ki = 180.0 nM 6.75
CHEMBL3409255 Ki = 220.0 nM 6.66
CHEMBL3409247 Ki = 270.0 nM 6.57
CHEMBL3409260 Ki = 290.0 nM 6.54