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Assay Detail

CHEMBL4046980

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

Binding
Displacement of [3H]prazosin from 5-sigma1 receptor in porcine cerebral cortex homogenates
21
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

β-Arrestin biased dopamine D2 receptor partial agonists: Synthesis and pharmacological evaluation.
Männel B, Hübner H, Möller D, Gmeiner P.
Bioorg Med Chem (2017) 25 : 5613 -5628
PubMed 28870802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.65 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4079375 1 7.96
CHEMBL4063145 2 7.89
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.77
CHEMBL4068561 2 7.54
CHEMBL4103639 1 7.31
CHEMBL4085752 2 7.05
CHEMBL4095881 1 6.80
CHEMBL4087217 1 6.80
CHEMBL4065797 1 6.05
CHEMBL4094407 1 5.82
CHEMBL4102646 1 5.82
CHEMBL4064759 1 5.62
CHEMBL4093493 1 5.38
CHEMBL4064191 1 4.92
CHEMBL4084712 1 4.89
CHEMBL4094900 1 -
CHEMBL4092462 1 -
CHEMBL4072785 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4079375 Ki = 11.0 nM 7.96
CHEMBL4063145 Ki = 13.0 nM 7.89
CHEMBL1112 ARIPIPRAZOLE Ki = 17.0 nM 7.77
CHEMBL4063145 Ki = 17.0 nM 7.77
CHEMBL4068561 Ki = 29.0 nM 7.54
CHEMBL4068561 Ki = 39.0 nM 7.41
CHEMBL4103639 Ki = 49.0 nM 7.31
CHEMBL4085752 Ki = 89.0 nM 7.05
CHEMBL4085752 Ki = 120.0 nM 6.92
CHEMBL4087217 Ki = 160.0 nM 6.80
CHEMBL4095881 Ki = 160.0 nM 6.80
CHEMBL4065797 Ki = 900.0 nM 6.05
CHEMBL4094407 Ki = 1500.0 nM 5.82
CHEMBL4102646 Ki = 1500.0 nM 5.82
CHEMBL4064759 Ki = 2400.0 nM 5.62
CHEMBL4093493 Ki = 4200.0 nM 5.38
CHEMBL4064191 Ki = 12000.0 nM 4.92
CHEMBL4084712 Ki = 13000.0 nM 4.89
CHEMBL4092462 Ki > 15000.0 nM -
CHEMBL4072785 Ki > 20000.0 nM -
CHEMBL4094900 Ki > 15000.0 nM -