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Assay Detail

CHEMBL1260560

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

Binding
Displacement of [3H]-8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.
Favor DA, Powers JJ, White AD, Fitzgerald LW, Groppi V, Serpa KA.
Bioorg Med Chem Lett (2010) 20 : 5666 -5669
PubMed 20801650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 9.56 10.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1258761 1 10.85
CHEMBL1258533 1 10.82
CHEMBL1258648 1 10.35
CHEMBL1258879 1 10.30
CHEMBL1258426 1 9.99
CHEMBL1257856 1 9.97
CHEMBL1258312 1 9.83
CHEMBL1258647 1 9.82
CHEMBL1257145 1 9.75
CHEMBL1258425 1 9.69
CHEMBL1258532 1 9.61
CHEMBL1257857 1 9.55
CHEMBL1258760 1 9.08
CHEMBL1257261 1 8.89
CHEMBL1258880 1 8.81
CHEMBL1257968 1 8.70
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.15
CHEMBL1257144 1 7.87
CHEMBL1257262 1 -
CHEMBL1257382 1 -
CHEMBL1257383 1 -
CHEMBL1257492 1 -
CHEMBL1257493 1 -
CHEMBL1257613 1 -
CHEMBL1257614 1 -
CHEMBL1257734 1 -
CHEMBL1257735 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1258761 Ki = 0.0141 nM 10.85
CHEMBL1258533 Ki = 0.0152 nM 10.82
CHEMBL1258648 Ki = 0.0447 nM 10.35
CHEMBL1258879 Ki = 0.0504 nM 10.30
CHEMBL1258426 Ki = 0.102 nM 9.99
CHEMBL1257856 Ki = 0.108 nM 9.97
CHEMBL1258312 Ki = 0.149 nM 9.83
CHEMBL1258647 Ki = 0.151 nM 9.82
CHEMBL1257145 Ki = 0.179 nM 9.75
CHEMBL1258425 Ki = 0.204 nM 9.69
CHEMBL1258532 Ki = 0.243 nM 9.61
CHEMBL1257857 Ki = 0.279 nM 9.55
CHEMBL1258760 Ki = 0.838 nM 9.08
CHEMBL1257261 Ki = 1.3 nM 8.89
CHEMBL1258880 Ki = 1.54 nM 8.81
CHEMBL1257968 Ki = 1.99 nM 8.70
CHEMBL1112 ARIPIPRAZOLE Ki = 7.0 nM 8.15
CHEMBL1257144 Ki = 13.4 nM 7.87
CHEMBL1257262 Ki - -
CHEMBL1257382 Ki - -
CHEMBL1257383 Ki - -
CHEMBL1257492 Ki - -
CHEMBL1257493 Ki - -
CHEMBL1257613 Ki - -
CHEMBL1257614 Ki - -
CHEMBL1257734 Ki - -
CHEMBL1257735 Ki - -