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Assay Detail

CHEMBL4394035

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

Binding
Displacement of [3H] raclopride from human recombinant D2L receptor expressed in HEK293 cells measured after 1 hr by microbeta scintillation counting method
29
Total Activities
29
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

Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT7 receptor low-basicity agonists, potential neuropathic painkillers.
Hogendorf AS, Hogendorf A, Popiołek-Barczyk K, Ciechanowska A, Mika J, Satała G, Walczak M, Latacz G, Handzlik J, Kieć-Kononowicz K, Ponimaskin E, Schade S, Zeug A, Bijata M, Kubicki M, Kurczab R, Lenda T, Staroń J, Bugno R, Duszyńska B, Pilarski B, Bojarski AJ.
Eur J Med Chem (2019) 170 : 261 -275
PubMed 30904783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 5.84 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL708 ZIPRASIDONE 4.0 1 9.05
CHEMBL4526012 1 5.73
CHEMBL4555349 1 5.52
CHEMBL4216263 1 5.31
CHEMBL4452569 1 5.15
CHEMBL4592256 1 5.06
CHEMBL4476372 1 5.03
CHEMBL4531898 1 -
CHEMBL4204595 1 -
CHEMBL4573883 1 -
CHEMBL4529615 1 -
CHEMBL4476520 1 -
CHEMBL4559312 1 -
CHEMBL4452121 1 -
CHEMBL4455588 1 -
CHEMBL4565881 1 -
CHEMBL4464377 1 -
CHEMBL4469847 1 -
CHEMBL4516621 1 -
CHEMBL4555115 1 -
CHEMBL4438349 1 -
CHEMBL4585956 1 -
CHEMBL4462820 1 -
CHEMBL4541526 1 -
CHEMBL4558202 1 -
CHEMBL4583507 1 -
CHEMBL4444268 1 -
CHEMBL4435235 1 -
CHEMBL4442337 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL708 ZIPRASIDONE Ki = 0.9 nM 9.05
CHEMBL4526012 Ki = 1862.0 nM 5.73
CHEMBL4555349 Ki = 3020.0 nM 5.52
CHEMBL4216263 Ki = 4898.0 nM 5.31
CHEMBL4452569 Ki = 7080.0 nM 5.15
CHEMBL4592256 Ki = 8710.0 nM 5.06
CHEMBL4476372 Ki = 9333.0 nM 5.03
CHEMBL4531898 Ki > 10000.0 nM -
CHEMBL4204595 Ki > 10000.0 nM -
CHEMBL4573883 Ki > 10000.0 nM -
CHEMBL4529615 Ki > 10000.0 nM -
CHEMBL4476520 Ki > 10000.0 nM -
CHEMBL4559312 Ki > 10000.0 nM -
CHEMBL4452121 Ki > 10000.0 nM -
CHEMBL4455588 Ki > 10000.0 nM -
CHEMBL4565881 Ki > 10000.0 nM -
CHEMBL4464377 Ki > 10000.0 nM -
CHEMBL4469847 Ki > 10000.0 nM -
CHEMBL4516621 Ki > 10000.0 nM -
CHEMBL4555115 Ki > 10000.0 nM -
CHEMBL4438349 Ki > 10000.0 nM -
CHEMBL4585956 Ki > 10000.0 nM -
CHEMBL4462820 Ki > 10000.0 nM -
CHEMBL4541526 Ki > 10000.0 nM -
CHEMBL4558202 Ki > 10000.0 nM -
CHEMBL4583507 Ki > 10000.0 nM -
CHEMBL4444268 Ki > 10000.0 nM -
CHEMBL4435235 Ki > 10000.0 nM -
CHEMBL4442337 Ki > 10000.0 nM -