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Assay Detail

CHEMBL1776016

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

Binding
Displacement of [3H]Spiperone from human dopamine D2L receptor expressed in CHO cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder.
Johnson DS, Choi C, Fay LK, Favor DA, Repine JT, White AD, Akunne HC, Fitzgerald L, Nicholls K, Snyder BJ, Whetzel SZ, Zhang L, Serpa KA.
Bioorg Med Chem Lett (2011) 21 : 2621 -2625
PubMed 21353774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 8.79 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774079 1 9.15
CHEMBL1774080 PF-00217830 2.0 1 9.09
CHEMBL1774063 1 9.00
CHEMBL1774064 1 9.00
CHEMBL1774085 1 9.00
CHEMBL1774066 1 9.00
CHEMBL1774069 1 9.00
CHEMBL1774078 1 9.00
CHEMBL1774073 1 9.00
CHEMBL1774074 1 9.00
CHEMBL1774076 1 9.00
CHEMBL1774082 1 8.96
CHEMBL1774086 1 8.92
CHEMBL1774077 1 8.85
CHEMBL1774081 1 8.80
CHEMBL1774087 1 8.77
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.74
CHEMBL1774083 1 8.70
CHEMBL1774065 1 8.70
CHEMBL1774071 1 8.60
CHEMBL1774068 1 8.60
CHEMBL1774062 1 8.59
CHEMBL1774075 1 8.52
CHEMBL1774072 1 8.52
CHEMBL1774070 1 8.30
CHEMBL1774067 1 8.24
CHEMBL1774084 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774079 Ki = 0.71 nM 9.15
CHEMBL1774080 PF-00217830 Ki = 0.81 nM 9.09
CHEMBL1774063 Ki = 1.0 nM 9.00
CHEMBL1774064 Ki = 1.0 nM 9.00
CHEMBL1774085 Ki = 1.0 nM 9.00
CHEMBL1774066 Ki = 1.0 nM 9.00
CHEMBL1774069 Ki = 1.0 nM 9.00
CHEMBL1774078 Ki = 1.0 nM 9.00
CHEMBL1774073 Ki = 1.0 nM 9.00
CHEMBL1774074 Ki = 1.0 nM 9.00
CHEMBL1774076 Ki = 1.0 nM 9.00
CHEMBL1774082 Ki = 1.1 nM 8.96
CHEMBL1774086 Ki = 1.2 nM 8.92
CHEMBL1774077 Ki = 1.4 nM 8.85
CHEMBL1774081 Ki = 1.6 nM 8.80
CHEMBL1774087 Ki = 1.7 nM 8.77
CHEMBL1112 ARIPIPRAZOLE Ki = 1.8 nM 8.74
CHEMBL1774083 Ki = 2.0 nM 8.70
CHEMBL1774065 Ki = 2.0 nM 8.70
CHEMBL1774071 Ki = 2.5 nM 8.60
CHEMBL1774068 Ki = 2.5 nM 8.60
CHEMBL1774062 Ki = 2.6 nM 8.59
CHEMBL1774075 Ki = 3.0 nM 8.52
CHEMBL1774072 Ki = 3.0 nM 8.52
CHEMBL1774070 Ki = 5.0 nM 8.30
CHEMBL1774067 Ki = 5.7 nM 8.24
CHEMBL1774084 Ki = 6.0 nM 8.22