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Assay Detail

CHEMBL671417

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

Binding
In vitro binding affinity at human Dopamine receptor D2 expressed in CHO K1 cells was measured by its ability to displace [3H]- N-0437
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety.
Dijkstra D, Rodenhuis N, Vermeulen ES, Pugsley TA, Wise LD, Wikström HV.
J Med Chem (2002) 45 : 3022 -3031
PubMed 12086487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.97 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1303 ROTIGOTINE 4.0 1 10.22
CHEMBL102582 1 8.21
CHEMBL15136 1 7.85
CHEMBL103622 1 7.70
CHEMBL103857 1 7.57
CHEMBL301559 1 7.47
CHEMBL322638 1 6.43
CHEMBL105623 1 6.36
CHEMBL102632 1 6.20
CHEMBL103441 1 5.97
CHEMBL104135 1 5.69
CHEMBL103912 1 5.51
CHEMBL102414 1 5.43
CHEMBL316584 1 -
CHEMBL319051 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1303 ROTIGOTINE Ki = 0.06 nM 10.22
CHEMBL102582 Ki = 6.24 nM 8.21
CHEMBL15136 Ki = 14.0 nM 7.85
CHEMBL103622 Ki = 20.0 nM 7.70
CHEMBL103857 Ki = 27.0 nM 7.57
CHEMBL301559 Ki = 34.0 nM 7.47
CHEMBL322638 Ki = 375.0 nM 6.43
CHEMBL105623 Ki = 439.0 nM 6.36
CHEMBL102632 Ki = 630.0 nM 6.20
CHEMBL103441 Ki = 1080.0 nM 5.97
CHEMBL104135 Ki = 2037.0 nM 5.69
CHEMBL103912 Ki = 3107.0 nM 5.51
CHEMBL102414 Ki = 3676.0 nM 5.43
CHEMBL316584 Ki > 3676.0 nM -
CHEMBL319051 Ki > 4780.0 nM -