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Assay Detail

CHEMBL3872756

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

Binding
Displacement of [3H]methyl-spiperone from recombinant human D3 receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL ↗
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics.
Chen XW, Sun YY, Fu L, Li JQ.
Eur J Med Chem (2016) 123 : 332 -353
PubMed 27487565 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 9.60 10.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3905247 — — 1 10.54
CHEMBL3918755 — — 1 10.37
CHEMBL3966842 — — 1 10.37
CHEMBL3895540 — — 1 10.34
CHEMBL3920252 — — 1 10.33
CHEMBL3932186 — — 1 10.29
CHEMBL3902496 — — 1 10.28
CHEMBL3896937 — — 1 10.26
CHEMBL3976282 — — 1 10.25
CHEMBL3982486 — — 1 10.24
CHEMBL3933256 — — 1 10.24
CHEMBL3948056 — — 1 10.21
CHEMBL3967779 — — 1 10.05
CHEMBL2028019 CARIPRAZINE 4.0 1 10.02
CHEMBL3892440 — — 1 10.02
CHEMBL3946995 — — 1 9.89
CHEMBL3962525 — — 1 9.85
CHEMBL3973487 — — 1 9.80
CHEMBL3940712 — — 1 9.74
CHEMBL3929168 — — 1 9.72
CHEMBL3956720 — — 1 9.68
CHEMBL3920432 — — 1 9.66
CHEMBL3970746 — — 1 9.62
CHEMBL3913691 — — 1 9.57
CHEMBL3938210 — — 1 9.51
CHEMBL3903560 — — 1 9.51
CHEMBL3960785 — — 1 9.40
CHEMBL3971907 — — 1 9.11
CHEMBL3959698 — — 1 9.00
CHEMBL3941190 — — 1 8.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3905247 — Ki = 0.029 nM 10.54
CHEMBL3918755 — Ki = 0.043 nM 10.37
CHEMBL3966842 — Ki = 0.043 nM 10.37
CHEMBL3895540 — Ki = 0.046 nM 10.34
CHEMBL3920252 — Ki = 0.047 nM 10.33
CHEMBL3932186 — Ki = 0.051 nM 10.29
CHEMBL3902496 — Ki = 0.052 nM 10.28
CHEMBL3896937 — Ki = 0.055 nM 10.26
CHEMBL3976282 — Ki = 0.056 nM 10.25
CHEMBL3982486 — Ki = 0.058 nM 10.24
CHEMBL3933256 — Ki = 0.058 nM 10.24
CHEMBL3948056 — Ki = 0.062 nM 10.21
CHEMBL3967779 — Ki = 0.09 nM 10.05
CHEMBL2028019 CARIPRAZINE Ki = 0.096 nM 10.02
CHEMBL3892440 — Ki = 0.095 nM 10.02
CHEMBL3946995 — Ki = 0.13 nM 9.89
CHEMBL3962525 — Ki = 0.14 nM 9.85
CHEMBL3973487 — Ki = 0.16 nM 9.80
CHEMBL3940712 — Ki = 0.18 nM 9.74
CHEMBL3929168 — Ki = 0.19 nM 9.72
CHEMBL3956720 — Ki = 0.21 nM 9.68
CHEMBL3920432 — Ki = 0.22 nM 9.66
CHEMBL3970746 — Ki = 0.24 nM 9.62
CHEMBL3913691 — Ki = 0.27 nM 9.57
CHEMBL3938210 — Ki = 0.31 nM 9.51
CHEMBL3903560 — Ki = 0.31 nM 9.51
CHEMBL3960785 — Ki = 0.4 nM 9.40
CHEMBL3971907 — Ki = 0.78 nM 9.11
CHEMBL3959698 — Ki = 1.0 nM 9.00
CHEMBL3941190 — Ki = 1.1 nM 8.96
CHEMBL3953773 — Ki = 1.2 nM 8.92
CHEMBL3900752 — Ki = 1.4 nM 8.85
CHEMBL3909821 — Ki = 1.6 nM 8.80
CHEMBL3923240 — Ki = 2.0 nM 8.70
CHEMBL3950977 — Ki = 2.3 nM 8.64
CHEMBL3942236 — Ki = 7.3 nM 8.14
CHEMBL3914241 — Ki = 8.7 nM 8.06
CHEMBL3891773 — Ki = 9.6 nM 8.02