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Assay Detail

CHEMBL4821476

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

Binding
Displacement of [3H]-raclopride from human D2R expressed in human HEK293 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.
Kułaga D, Jaśkowska J, Satała G.
Bioorg Med Chem Lett (2021) 42 : 128028 -128028
PubMed 33839253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.24 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4565558 1 9.00
CHEMBL4876545 1 8.70
CHEMBL4869198 1 7.77
CHEMBL4866981 1 7.70
CHEMBL4860754 1 7.70
CHEMBL4860626 1 7.58
CHEMBL4874914 1 7.47
CHEMBL394110 1 7.42
CHEMBL4470487 1 7.29
CHEMBL4853700 1 7.04
CHEMBL238916 1 6.95
CHEMBL4872713 1 6.78
CHEMBL238915 1 6.75
CHEMBL4867109 1 6.59
CHEMBL238917 1 6.44
CHEMBL4873100 1 6.02
CHEMBL8412 IPSAPIRONE 2.0 1 5.91
CHEMBL4853248 1 -
CHEMBL2107024 REVOSPIRONE 2.0 1 -
CHEMBL4849583 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4565558 Ki = 1.0 nM 9.00
CHEMBL4876545 Ki = 2.0 nM 8.70
CHEMBL4869198 Ki = 17.0 nM 7.77
CHEMBL4866981 Ki = 20.0 nM 7.70
CHEMBL4860754 Ki = 20.0 nM 7.70
CHEMBL4860626 Ki = 26.0 nM 7.58
CHEMBL4874914 Ki = 34.0 nM 7.47
CHEMBL394110 Ki = 38.0 nM 7.42
CHEMBL4470487 Ki = 51.0 nM 7.29
CHEMBL4853700 Ki = 92.0 nM 7.04
CHEMBL238916 Ki = 113.0 nM 6.95
CHEMBL4872713 Ki = 165.0 nM 6.78
CHEMBL238915 Ki = 177.0 nM 6.75
CHEMBL4867109 Ki = 254.0 nM 6.59
CHEMBL238917 Ki = 360.0 nM 6.44
CHEMBL4873100 Ki = 954.0 nM 6.02
CHEMBL8412 IPSAPIRONE Ki = 1224.0 nM 5.91
CHEMBL4853248 Ki - -
CHEMBL2107024 REVOSPIRONE Ki - -
CHEMBL4849583 Ki - -