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Assay Detail

CHEMBL666355

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

Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor.
DeNinno MP, Schoenleber R, Perner RJ, Lijewski L, Asin KE, Britton DR, MacKenzie R, Kebabian JW.
J Med Chem (1991) 34 : 2561 -2569
PubMed 1652023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.69 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87734 1 9.31
CHEMBL86931 1 8.80
CHEMBL315468 1 8.52
CHEMBL314459 1 8.27
CHEMBL313304 1 7.86
CHEMBL315750 1 7.85
CHEMBL85409 1 7.52
CHEMBL82899 1 7.50
CHEMBL313530 1 7.50
CHEMBL415080 1 7.28
CHEMBL24077 (R)-SKF-38393 1 7.19
CHEMBL85689 1 7.05
CHEMBL2115213 1 6.78
CHEMBL84983 1 6.61
CHEMBL315005 1 6.51
CHEMBL86669 1 6.48
CHEMBL86576 1 6.43
CHEMBL315849 1 6.39
CHEMBL87910 1 6.35
CHEMBL420604 1 6.32
CHEMBL87172 1 6.28
CHEMBL420972 1 6.15
CHEMBL431220 1 6.06
CHEMBL87958 1 5.99
CHEMBL419680 1 5.81
CHEMBL2114209 1 5.75
CHEMBL86325 1 5.64
CHEMBL315535 1 5.60
CHEMBL87897 1 5.58
CHEMBL85552 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87734 Ki = 0.49 nM 9.31
CHEMBL86931 Ki = 1.6 nM 8.80
CHEMBL315468 Ki = 3.0 nM 8.52
CHEMBL314459 Ki = 5.4 nM 8.27
CHEMBL313304 Ki = 13.7 nM 7.86
CHEMBL315750 Ki = 14.1 nM 7.85
CHEMBL85409 Ki = 30.4 nM 7.52
CHEMBL82899 Ki = 31.8 nM 7.50
CHEMBL313530 Ki = 31.7 nM 7.50
CHEMBL415080 Ki = 52.0 nM 7.28
CHEMBL24077 (R)-SKF-38393 Ki = 64.1 nM 7.19
CHEMBL85689 Ki = 88.7 nM 7.05
CHEMBL2115213 Ki = 167.0 nM 6.78
CHEMBL84983 Ki = 248.0 nM 6.61
CHEMBL315005 Ki = 310.0 nM 6.51
CHEMBL86669 Ki = 329.0 nM 6.48
CHEMBL86576 Ki = 374.0 nM 6.43
CHEMBL315849 Ki = 407.0 nM 6.39
CHEMBL87910 Ki = 443.0 nM 6.35
CHEMBL420604 Ki = 479.0 nM 6.32
CHEMBL87172 Ki = 530.0 nM 6.28
CHEMBL420972 Ki = 704.0 nM 6.15
CHEMBL431220 Ki = 870.0 nM 6.06
CHEMBL87958 Ki = 1030.0 nM 5.99
CHEMBL419680 Ki = 1540.0 nM 5.81
CHEMBL2114209 Ki = 1760.0 nM 5.75
CHEMBL86325 Ki = 2290.0 nM 5.64
CHEMBL315535 Ki = 2510.0 nM 5.60
CHEMBL87897 Ki = 2650.0 nM 5.58
CHEMBL85552 Ki = 3140.0 nM 5.50
CHEMBL84557 Ki = 3190.0 nM 5.50
CHEMBL420788 Ki = 4730.0 nM 5.33
CHEMBL83080 Ki = 7200.0 nM 5.14
CHEMBL315516 Ki > 10000.0 nM -