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Assay Detail

CHEMBL673002

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

Binding
Dopaminergic activity assessed in vitro for displacement of [3H]apomorphine from specific binding sites on rat striatal membranes
28
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists.
Jones JH, Anderson PS, Baldwin JJ, Clineschmidt BV, McClure DE, Lundell GF, Randall WC, Martin GE, Williams M, Hirshfield JM.
J Med Chem (1984) 27 : 1607 -1613
PubMed 6094811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.49 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 8.96
CHEMBL44558 1 8.70
CHEMBL531 PERGOLIDE 4.0 1 8.51
CHEMBL42242 1 8.48
CHEMBL41980 1 7.85
CHEMBL42309 1 7.85
CHEMBL44501 4 7.71
CHEMBL493 BROMOCRIPTINE 4.0 1 7.55
CHEMBL41420 1 7.09
CHEMBL43071 1 6.96
CHEMBL295359 1 6.92
CHEMBL42237 1 6.74
CHEMBL42909 1 6.73
CHEMBL40542 1 6.38
CHEMBL44257 1 6.24
CHEMBL42291 1 5.91
CHEMBL43762 4 5.82
CHEMBL288531 1 5.53
CHEMBL42047 1 5.42
CHEMBL288765 1 5.33
CHEMBL44528 1 5.08
CHEMBL43930 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE IC50 = 1.1 nM 8.96
CHEMBL44558 IC50 = 2.0 nM 8.70
CHEMBL531 PERGOLIDE IC50 = 3.1 nM 8.51
CHEMBL42242 IC50 = 3.3 nM 8.48
CHEMBL41980 IC50 = 14.0 nM 7.85
CHEMBL42309 IC50 = 14.0 nM 7.85
CHEMBL44501 IC50 = 19.6 nM 7.71
CHEMBL44501 IC50 = 23.0 nM 7.64
CHEMBL493 BROMOCRIPTINE IC50 = 27.9 nM 7.55
CHEMBL41420 IC50 = 82.0 nM 7.09
CHEMBL43071 IC50 = 110.0 nM 6.96
CHEMBL295359 IC50 = 120.0 nM 6.92
CHEMBL42237 IC50 = 182.0 nM 6.74
CHEMBL42909 IC50 = 185.0 nM 6.73
CHEMBL40542 IC50 = 421.0 nM 6.38
CHEMBL44257 IC50 = 572.0 nM 6.24
CHEMBL42291 IC50 = 1242.0 nM 5.91
CHEMBL43762 IC50 = 1520.0 nM 5.82
CHEMBL43762 IC50 = 2370.0 nM 5.62
CHEMBL288531 IC50 = 2930.0 nM 5.53
CHEMBL42047 IC50 = 3800.0 nM 5.42
CHEMBL288765 IC50 = 4730.0 nM 5.33
CHEMBL44528 IC50 = 8300.0 nM 5.08
CHEMBL43762 IC50 = 10210.0 nM 4.99
CHEMBL44501 IC50 = 19600.0 nM 4.71
CHEMBL44501 IC50 = 25300.0 nM 4.60
CHEMBL43930 IC50 = 62400.0 nM 4.21
CHEMBL43762 IC50 = 65300.0 nM 4.18