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Assay Detail

CHEMBL670611

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

Binding
Ability to inhibit the binding of [3H]spiroperidol in rat striatal tissue
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and neuroleptic activity of 3-(1-substituted-4-piperidinyl)-1,2-benzisoxazoles.
Strupczewski JT, Allen RC, Gardner BA, Schmid BL, Stache U, Glamkowski EJ, Jones MC, Ellis DB, Huger FP, Dunn RW.
J Med Chem (1985) 28 : 761 -769
PubMed 2861286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.88 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164940 1 8.17
CHEMBL350575 1 7.92
CHEMBL168104 1 7.89
CHEMBL351954 1 7.70
CHEMBL165301 1 7.60
CHEMBL54 HALOPERIDOL 4.0 1 7.39
CHEMBL165775 1 7.38
CHEMBL166095 1 7.33
CHEMBL165857 1 7.17
CHEMBL166311 1 7.16
CHEMBL349840 1 7.16
CHEMBL344115 1 7.11
CHEMBL71 CHLORPROMAZINE 4.0 1 7.11
CHEMBL165576 1 7.06
CHEMBL349632 1 6.85
CHEMBL164973 1 6.85
CHEMBL351707 1 6.82
CHEMBL163680 1 6.82
CHEMBL166298 1 6.72
CHEMBL164679 1 6.70
CHEMBL163832 1 6.57
CHEMBL165133 1 6.47
CHEMBL350957 1 6.38
CHEMBL354250 1 6.38
CHEMBL165797 1 6.24
CHEMBL167086 1 5.96
CHEMBL165077 1 5.55
CHEMBL163656 1 5.55
CHEMBL164584 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164940 IC50 = 6.7 nM 8.17
CHEMBL350575 IC50 = 12.0 nM 7.92
CHEMBL168104 IC50 = 13.0 nM 7.89
CHEMBL351954 IC50 = 20.0 nM 7.70
CHEMBL165301 IC50 = 25.0 nM 7.60
CHEMBL54 HALOPERIDOL IC50 = 41.0 nM 7.39
CHEMBL165775 IC50 = 42.0 nM 7.38
CHEMBL166095 IC50 = 47.0 nM 7.33
CHEMBL165857 IC50 = 68.0 nM 7.17
CHEMBL166311 IC50 = 69.0 nM 7.16
CHEMBL349840 IC50 = 70.0 nM 7.16
CHEMBL344115 IC50 = 78.0 nM 7.11
CHEMBL71 CHLORPROMAZINE IC50 = 77.0 nM 7.11
CHEMBL165576 IC50 = 88.0 nM 7.06
CHEMBL349632 IC50 = 140.0 nM 6.85
CHEMBL164973 IC50 = 140.0 nM 6.85
CHEMBL351707 IC50 = 150.0 nM 6.82
CHEMBL163680 IC50 = 150.0 nM 6.82
CHEMBL166298 IC50 = 190.0 nM 6.72
CHEMBL164679 IC50 = 200.0 nM 6.70
CHEMBL163832 IC50 = 270.0 nM 6.57
CHEMBL165133 IC50 = 340.0 nM 6.47
CHEMBL350957 IC50 = 420.0 nM 6.38
CHEMBL354250 IC50 = 420.0 nM 6.38
CHEMBL165797 IC50 = 580.0 nM 6.24
CHEMBL167086 IC50 = 1100.0 nM 5.96
CHEMBL165077 IC50 = 2800.0 nM 5.55
CHEMBL163656 IC50 = 2800.0 nM 5.55
CHEMBL164584 IC50 = 3800.0 nM 5.42