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Assay Detail

CHEMBL673066

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

Binding
Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand.
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Binding and preliminary evaluation of 5-hydroxy- and 10-hydroxy-2,3, 12,12a-tetrahydro-1H-[1]benzoxepino[2,3,4-ij]isoquinolines as dopamine receptor ligands.
Claudi F, Di Stefano A, Napolitani F, Cingolani GM, Giorgioni G, Fontenla JA, Montenegro GY, Rivas ME, Rosa E, Michelotto B, Orlando G, Brunetti L.
J Med Chem (2000) 43 : 599 -608
PubMed 10691686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 5.96 8.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.67
CHEMBL53 APOMORPHINE 4.0 1 7.26
CHEMBL155208 1 6.56
CHEMBL59 DOPAMINE 4.0 1 6.14
CHEMBL155352 1 6.14
CHEMBL156011 1 6.07
CHEMBL157799 1 5.91
CHEMBL350471 1 5.74
CHEMBL348465 1 5.73
CHEMBL422169 1 5.66
CHEMBL347243 1 5.51
CHEMBL346792 1 5.46
CHEMBL439639 1 5.19
CHEMBL158067 1 5.15
CHEMBL155002 1 5.07
CHEMBL154948 1 5.03
CHEMBL155066 1 -
CHEMBL436042 1 -
CHEMBL345240 1 -
CHEMBL155351 1 -
CHEMBL154468 1 -
CHEMBL349311 1 -
CHEMBL154015 1 -
CHEMBL154301 1 -
CHEMBL350457 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.138 nM 8.67
CHEMBL53 APOMORPHINE Ki = 54.95 nM 7.26
CHEMBL155208 Ki = 275.42 nM 6.56
CHEMBL59 DOPAMINE Ki = 724.44 nM 6.14
CHEMBL155352 Ki = 724.44 nM 6.14
CHEMBL156011 Ki = 851.14 nM 6.07
CHEMBL157799 Ki = 1230.27 nM 5.91
CHEMBL350471 Ki = 1819.7 nM 5.74
CHEMBL348465 Ki = 1862.09 nM 5.73
CHEMBL422169 Ki = 2187.76 nM 5.66
CHEMBL347243 Ki = 3090.3 nM 5.51
CHEMBL346792 Ki = 3467.37 nM 5.46
CHEMBL439639 Ki = 6456.54 nM 5.19
CHEMBL158067 Ki = 7079.46 nM 5.15
CHEMBL155002 Ki = 8511.38 nM 5.07
CHEMBL154948 Ki = 9332.54 nM 5.03
CHEMBL155066 Ki < 10000.0 nM -
CHEMBL436042 Ki < 10000.0 nM -
CHEMBL345240 Ki < 10000.0 nM -
CHEMBL155351 Ki < 10000.0 nM -
CHEMBL154468 Ki < 10000.0 nM -
CHEMBL349311 Ki < 10000.0 nM -
CHEMBL154015 Ki < 10000.0 nM -
CHEMBL154301 Ki < 10000.0 nM -
CHEMBL350457 Ki < 10000.0 nM -