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Assay Detail

CHEMBL671741

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

Binding
In vitro ability to displace [3H]spiperone binding from dopamine receptor D2 in rat striatal membrane.
29
Total Activities
29
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

Conformationally constrained butyrophenones with mixed dopaminergic (D(2)) and serotoninergic (5-HT(2A), 5-HT(2C)) affinities: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl)benzo- and -thienocycloalkanones as putative atypical antipsychotics.
Raviña E, Negreira J, Cid J, Masaguer CF, Rosa E, Rivas ME, Fontenla JA, Loza MI, Tristán H, Cadavid MI, Sanz F, Lozoya E, Carotti A, Carrieri A.
J Med Chem (1999) 42 : 2774 -2797
PubMed 10425088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.15 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62 SCH-23390 1 9.27
CHEMBL54 HALOPERIDOL 4.0 1 8.48
CHEMBL310153 1 8.19
CHEMBL85 RISPERIDONE 4.0 1 8.09
CHEMBL554199 1 7.70
CHEMBL308480 1 7.68
CHEMBL92145 1 7.64
CHEMBL310734 1 7.60
CHEMBL541842 1 7.36
CHEMBL543613 1 7.34
CHEMBL87026 1 7.33
CHEMBL87943 1 7.32
CHEMBL539544 1 7.26
CHEMBL95098 1 7.17
CHEMBL87717 1 7.15
CHEMBL96781 1 7.04
CHEMBL540822 1 6.79
CHEMBL558817 1 6.76
CHEMBL544091 1 6.68
CHEMBL545488 1 6.65
CHEMBL95112 1 6.58
CHEMBL42 CLOZAPINE 4.0 1 6.58
CHEMBL542428 1 6.57
CHEMBL544319 1 6.50
CHEMBL544089 1 6.49
CHEMBL544318 1 6.49
CHEMBL92673 1 6.39
CHEMBL542181 1 6.19
CHEMBL545727 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62 SCH-23390 Ki = 0.537 nM 9.27
CHEMBL54 HALOPERIDOL Ki = 3.311 nM 8.48
CHEMBL310153 Ki = 6.457 nM 8.19
CHEMBL85 RISPERIDONE Ki = 8.128 nM 8.09
CHEMBL554199 Ki = 19.95 nM 7.70
CHEMBL308480 Ki = 20.89 nM 7.68
CHEMBL92145 Ki = 22.91 nM 7.64
CHEMBL310734 Ki = 25.12 nM 7.60
CHEMBL541842 Ki = 43.65 nM 7.36
CHEMBL543613 Ki = 45.71 nM 7.34
CHEMBL87026 Ki = 46.77 nM 7.33
CHEMBL87943 Ki = 47.86 nM 7.32
CHEMBL539544 Ki = 54.95 nM 7.26
CHEMBL95098 Ki = 67.61 nM 7.17
CHEMBL87717 Ki = 70.79 nM 7.15
CHEMBL96781 Ki = 91.2 nM 7.04
CHEMBL540822 Ki = 162.18 nM 6.79
CHEMBL558817 Ki = 173.78 nM 6.76
CHEMBL544091 Ki = 208.93 nM 6.68
CHEMBL545488 Ki = 223.87 nM 6.65
CHEMBL95112 Ki = 263.03 nM 6.58
CHEMBL42 CLOZAPINE Ki = 263.03 nM 6.58
CHEMBL542428 Ki = 269.15 nM 6.57
CHEMBL544319 Ki = 316.23 nM 6.50
CHEMBL544089 Ki = 323.59 nM 6.49
CHEMBL544318 Ki = 323.59 nM 6.49
CHEMBL92673 Ki = 407.38 nM 6.39
CHEMBL542181 Ki = 645.65 nM 6.19
CHEMBL545727 Ki = 1047.13 nM 5.98