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Assay Detail

CHEMBL4229834

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

Binding
Displacement of [3H]-ketanserin from human 5-HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs 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 CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL224) ↗
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 7.34 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 1 9.30
CHEMBL708 ZIPRASIDONE 4.0 1 8.77
CHEMBL715 OLANZAPINE 4.0 1 8.40
CHEMBL4250475 — — 1 8.30
CHEMBL4245263 — — 1 8.22
CHEMBL4243932 — — 1 8.15
CHEMBL4244691 — — 1 8.05
CHEMBL4239823 — — 1 8.05
CHEMBL4238679 — — 1 8.00
CHEMBL4241050 — — 1 7.92
CHEMBL42 CLOZAPINE 4.0 1 7.89
CHEMBL4246655 — — 1 7.89
CHEMBL4239091 — — 1 7.82
CHEMBL4239705 — — 1 7.80
CHEMBL4246202 — — 1 7.80
CHEMBL4242392 — — 1 7.75
CHEMBL4238479 — — 1 7.72
CHEMBL4242858 — — 1 7.68
CHEMBL4243497 — — 1 7.62
CHEMBL4250274 — — 1 7.58
CHEMBL4248491 — — 1 7.58
CHEMBL4245607 — — 1 7.54
CHEMBL4241081 — — 1 7.54
CHEMBL4238897 — — 1 7.52
CHEMBL4240162 — — 1 7.52
CHEMBL4249640 — — 1 7.48
CHEMBL4248544 — — 1 7.46
CHEMBL4240642 — — 1 7.46
CHEMBL4240954 — — 1 7.44
CHEMBL4243579 — — 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 0.5 nM 9.30
CHEMBL708 ZIPRASIDONE Ki = 1.7 nM 8.77
CHEMBL715 OLANZAPINE Ki = 4.0 nM 8.40
CHEMBL4250475 — Ki = 5.0 nM 8.30
CHEMBL4245263 — Ki = 6.0 nM 8.22
CHEMBL4243932 — Ki = 7.0 nM 8.15
CHEMBL4244691 — Ki = 9.0 nM 8.05
CHEMBL4239823 — Ki = 9.0 nM 8.05
CHEMBL4238679 — Ki = 10.0 nM 8.00
CHEMBL4241050 — Ki = 12.0 nM 7.92
CHEMBL42 CLOZAPINE Ki = 13.0 nM 7.89
CHEMBL4246655 — Ki = 13.0 nM 7.89
CHEMBL4239091 — Ki = 15.0 nM 7.82
CHEMBL4246202 — Ki = 16.0 nM 7.80
CHEMBL4239705 — Ki = 16.0 nM 7.80
CHEMBL4242392 — Ki = 18.0 nM 7.75
CHEMBL4238479 — Ki = 19.0 nM 7.72
CHEMBL4242858 — Ki = 21.0 nM 7.68
CHEMBL4243497 — Ki = 24.0 nM 7.62
CHEMBL4250274 — Ki = 26.0 nM 7.58
CHEMBL4248491 — Ki = 26.0 nM 7.58
CHEMBL4245607 — Ki = 29.0 nM 7.54
CHEMBL4241081 — Ki = 29.0 nM 7.54
CHEMBL4238897 — Ki = 30.0 nM 7.52
CHEMBL4240162 — Ki = 30.0 nM 7.52
CHEMBL4249640 — Ki = 33.0 nM 7.48
CHEMBL4240642 — Ki = 35.0 nM 7.46
CHEMBL4248544 — Ki = 35.0 nM 7.46
CHEMBL4240954 — Ki = 36.0 nM 7.44
CHEMBL4243579 — Ki = 41.0 nM 7.39
CHEMBL4249179 — Ki = 49.0 nM 7.31
CHEMBL4241497 — Ki = 51.0 nM 7.29
CHEMBL4243848 — Ki = 56.0 nM 7.25
CHEMBL1112 ARIPIPRAZOLE Ki = 63.0 nM 7.20
CHEMBL4244280 — Ki = 64.0 nM 7.19
CHEMBL4245997 — Ki = 76.0 nM 7.12
CHEMBL4242170 — Ki = 82.0 nM 7.09
CHEMBL54 HALOPERIDOL Ki = 89.0 nM 7.05
CHEMBL4247770 — Ki = 91.0 nM 7.04
CHEMBL4241830 — Ki = 110.0 nM 6.96
CHEMBL4250244 — Ki = 238.0 nM 6.62
CHEMBL4238029 — Ki = 244.0 nM 6.61
CHEMBL4238124 — Ki = 296.0 nM 6.53
CHEMBL4242268 — Ki = 390.0 nM 6.41
CHEMBL4248597 — Ki = 451.0 nM 6.35
CHEMBL4245622 — Ki = 1150.0 nM 5.94
CHEMBL4249426 — Ki = 1400.0 nM 5.85
CHEMBL4246630 — Ki = 1904.0 nM 5.72
CHEMBL4243036 — Ki = 1970.0 nM 5.71
CHEMBL4247275 — Ki = 2040.0 nM 5.69