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Assay Detail

CHEMBL4229838

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

Binding
Displacement of [3H]-raclopride from human D2LR expressed in HEK293 cell membranes after 1 hr at 37 degC by microbeta counting method
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.
Zajdel P, Kos T, Marciniec K, Satała G, Canale V, Kamiński K, Hołuj M, Lenda T, Koralewski R, Bednarski M, Nowiński L, Wójcikowski J, Daniel WA, Nikiforuk A, Nalepa I, Chmielarz P, Kuśmierczyk J, Bojarski AJ, Popik P.
Eur J Med Chem (2018) 145 : 790 -804
PubMed 29407591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 51 8.31 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4245263 — — 1 10.00
CHEMBL4246655 — — 1 9.85
CHEMBL4239091 — — 1 9.52
CHEMBL4242392 — — 1 9.30
CHEMBL85 RISPERIDONE 4.0 1 9.22
CHEMBL4242858 — — 1 9.15
CHEMBL1112 ARIPIPRAZOLE 4.0 1 9.10
CHEMBL708 ZIPRASIDONE 4.0 1 9.10
CHEMBL4238679 — — 1 9.05
CHEMBL4246202 — — 1 9.00
CHEMBL4241050 — — 1 8.77
CHEMBL54 HALOPERIDOL 4.0 1 8.70
CHEMBL4250475 — — 1 8.70
CHEMBL4249640 — — 1 8.52
CHEMBL4243579 — — 1 8.52
CHEMBL4245997 — — 1 8.52
CHEMBL4250274 — — 1 8.52
CHEMBL715 OLANZAPINE 4.0 1 8.40
CHEMBL4240162 — — 1 8.40
CHEMBL4249179 — — 1 8.40
CHEMBL4243848 — — 1 8.40
CHEMBL4244691 — — 1 8.30
CHEMBL4247275 — — 1 8.30
CHEMBL4238479 — — 1 8.30
CHEMBL4240642 — — 1 8.30
CHEMBL4248491 — — 1 8.22
CHEMBL4245607 — — 1 8.22
CHEMBL4241081 — — 1 8.15
CHEMBL4248597 — — 1 8.10
CHEMBL4240910 — — 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4245263 — Ki = 0.1 nM 10.00
CHEMBL4246655 — Ki = 0.14 nM 9.85
CHEMBL4239091 — Ki = 0.3 nM 9.52
CHEMBL4242392 — Ki = 0.5 nM 9.30
CHEMBL85 RISPERIDONE Ki = 0.6 nM 9.22
CHEMBL4242858 — Ki = 0.7 nM 9.15
CHEMBL1112 ARIPIPRAZOLE Ki = 0.8 nM 9.10
CHEMBL708 ZIPRASIDONE Ki = 0.8 nM 9.10
CHEMBL4238679 — Ki = 0.9 nM 9.05
CHEMBL4246202 — Ki = 1.0 nM 9.00
CHEMBL4241050 — Ki = 1.7 nM 8.77
CHEMBL54 HALOPERIDOL Ki = 2.0 nM 8.70
CHEMBL4250475 — Ki = 2.0 nM 8.70
CHEMBL4245997 — Ki = 3.0 nM 8.52
CHEMBL4243579 — Ki = 3.0 nM 8.52
CHEMBL4249640 — Ki = 3.0 nM 8.52
CHEMBL4250274 — Ki = 3.0 nM 8.52
CHEMBL715 OLANZAPINE Ki = 4.0 nM 8.40
CHEMBL4240162 — Ki = 4.0 nM 8.40
CHEMBL4249179 — Ki = 4.0 nM 8.40
CHEMBL4243848 — Ki = 4.0 nM 8.40
CHEMBL4244691 — Ki = 5.0 nM 8.30
CHEMBL4247275 — Ki = 5.0 nM 8.30
CHEMBL4238479 — Ki = 5.0 nM 8.30
CHEMBL4240642 — Ki = 5.0 nM 8.30
CHEMBL4248491 — Ki = 6.0 nM 8.22
CHEMBL4245607 — Ki = 6.0 nM 8.22
CHEMBL4241081 — Ki = 7.0 nM 8.15
CHEMBL4248597 — Ki = 8.0 nM 8.10
CHEMBL4240910 — Ki = 9.0 nM 8.05
CHEMBL4243497 — Ki = 10.0 nM 8.00
CHEMBL4241497 — Ki = 10.0 nM 8.00
CHEMBL4249426 — Ki = 11.0 nM 7.96
CHEMBL4238897 — Ki = 11.0 nM 7.96
CHEMBL4239823 — Ki = 11.0 nM 7.96
CHEMBL4246630 — Ki = 12.0 nM 7.92
CHEMBL4243036 — Ki = 12.0 nM 7.92
CHEMBL4238124 — Ki = 12.0 nM 7.92
CHEMBL4250244 — Ki = 13.0 nM 7.89
CHEMBL4241830 — Ki = 13.0 nM 7.89
CHEMBL4245622 — Ki = 15.0 nM 7.82
CHEMBL4240954 — Ki = 16.0 nM 7.80
CHEMBL4247770 — Ki = 19.0 nM 7.72
CHEMBL4248544 — Ki = 21.0 nM 7.68
CHEMBL4242268 — Ki = 22.0 nM 7.66
CHEMBL4244280 — Ki = 23.0 nM 7.64
CHEMBL4243932 — Ki = 24.0 nM 7.62
CHEMBL4239705 — Ki = 29.0 nM 7.54
CHEMBL4242170 — Ki = 37.0 nM 7.43
CHEMBL4238029 — Ki = 42.0 nM 7.38