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Assay Detail

CHEMBL670674

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

Binding
In vitro binding affinity against Dopamine receptor D2 like from rat caudate membrane using [3H]-spiperone as radioligand
39
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.
Michaelides MR, Hong Y, DiDomenico S, Bayburt EK, Asin KE, Britton DR, Lin CW, Shiosaki K.
J Med Chem (1997) 40 : 1585 -1599
PubMed 9171869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 6.03 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542351 1 7.29
CHEMBL41238 1 7.00
CHEMBL290842 1 6.84
CHEMBL44414 1 6.84
CHEMBL40667 1 6.82
CHEMBL41132 1 6.69
CHEMBL2114440 1 6.62
CHEMBL39266 1 6.52
CHEMBL288536 1 6.47
CHEMBL2114444 1 6.46
CHEMBL289867 1 6.35
CHEMBL289927 1 6.27
CHEMBL287931 1 6.25
CHEMBL2115377 2 6.19
CHEMBL28338 A-86929 -1.0 1 6.10
CHEMBL291100 1 6.04
CHEMBL2115372 2 6.01
CHEMBL554571 1 5.99
CHEMBL40950 1 5.89
CHEMBL417164 1 5.88
CHEMBL2114441 1 5.86
CHEMBL25856 DIHYDREXIDINE 2.0 1 5.85
CHEMBL2115374 2 5.85
CHEMBL41196 1 5.82
CHEMBL446350 1 5.76
CHEMBL291143 1 5.75
CHEMBL41809 1 5.75
CHEMBL38757 1 5.68
CHEMBL43514 1 5.59
CHEMBL288846 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542351 Ki = 51.0 nM 7.29
CHEMBL41238 Ki = 100.0 nM 7.00
CHEMBL290842 Ki = 145.0 nM 6.84
CHEMBL44414 Ki = 145.0 nM 6.84
CHEMBL40667 Ki = 150.0 nM 6.82
CHEMBL41132 Ki = 205.0 nM 6.69
CHEMBL2114440 Ki = 240.0 nM 6.62
CHEMBL39266 Ki = 300.0 nM 6.52
CHEMBL288536 Ki = 340.0 nM 6.47
CHEMBL2114444 Ki = 345.0 nM 6.46
CHEMBL289867 Ki = 450.0 nM 6.35
CHEMBL289927 Ki = 540.0 nM 6.27
CHEMBL287931 Ki = 560.0 nM 6.25
CHEMBL2115377 Ki = 640.0 nM 6.19
CHEMBL28338 A-86929 Ki = 800.0 nM 6.10
CHEMBL291100 Ki = 910.0 nM 6.04
CHEMBL2115372 Ki = 980.0 nM 6.01
CHEMBL554571 Ki = 1030.0 nM 5.99
CHEMBL40950 Ki = 1290.0 nM 5.89
CHEMBL417164 Ki = 1320.0 nM 5.88
CHEMBL2114441 Ki = 1380.0 nM 5.86
CHEMBL25856 DIHYDREXIDINE Ki = 1400.0 nM 5.85
CHEMBL2115374 Ki = 1400.0 nM 5.85
CHEMBL41196 Ki = 1530.0 nM 5.82
CHEMBL446350 Ki = 1720.0 nM 5.76
CHEMBL41809 Ki = 1760.0 nM 5.75
CHEMBL291143 Ki = 1800.0 nM 5.75
CHEMBL38757 Ki = 2090.0 nM 5.68
CHEMBL288846 Ki = 2560.0 nM 5.59
CHEMBL43514 Ki = 2590.0 nM 5.59
CHEMBL542593 Ki = 2800.0 nM 5.55
CHEMBL24077 (R)-SKF-38393 Ki = 2900.0 nM 5.54
CHEMBL290149 Ki = 3110.0 nM 5.51
CHEMBL2115373 Ki = 3260.0 nM 5.49
CHEMBL2115373 Ki = 4490.0 nM 5.35
CHEMBL2115372 Ki = 4790.0 nM 5.32
CHEMBL2115374 Ki = 5400.0 nM 5.27
CHEMBL2115377 Ki = 5450.0 nM 5.26
CHEMBL416435 Ki > 10000.0 nM -