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Assay Detail

CHEMBL671379

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

Binding
Binding affinity against cloned human Dopamine receptor D2 using [3H]spiperone as radioligand transfected in HEK cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431).
Michaelides MR, Hong Y, DiDomenico S, Asin KE, Britton DR, Lin CW, Williams M, Shiosaki K.
J Med Chem (1995) 38 : 3445 -3447
PubMed 7658429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.85 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59 DOPAMINE 4.0 1 6.58
CHEMBL28338 A-86929 -1.0 1 6.15
CHEMBL25856 DIHYDREXIDINE 2.0 1 5.82
CHEMBL291143 1 5.81
CHEMBL544814 1 5.40
CHEMBL24077 (R)-SKF-38393 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59 DOPAMINE Ki = 260.0 nM 6.58
CHEMBL28338 A-86929 Ki = 710.0 nM 6.15
CHEMBL25856 DIHYDREXIDINE Ki = 1520.0 nM 5.82
CHEMBL291143 Ki = 1550.0 nM 5.81
CHEMBL544814 Ki = 4020.0 nM 5.40
CHEMBL24077 (R)-SKF-38393 Ki = 4670.0 nM 5.33