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Assay Detail

CHEMBL897620

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

Binding
Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells
43
Total Activities
43
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 Intermediate

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Hybrid approach for the design of highly affine and selective dopamine D(3) receptor ligands using privileged scaffolds of biogenic amine GPCR ligands.
Sasse BC, Mach UR, Leppaenen J, Calmels T, Stark H.
Bioorg Med Chem (2007) 15 : 7258 -7273
PubMed 17826096 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 7.66 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239923 1 9.52
CHEMBL25236 BP-897 1 9.04
CHEMBL241455 1 8.62
CHEMBL239706 1 8.57
CHEMBL394019 1 8.55
CHEMBL240600 1 8.44
CHEMBL239493 1 8.22
CHEMBL241026 1 8.21
CHEMBL240589 1 8.06
CHEMBL241226 1 7.97
CHEMBL240588 1 7.96
CHEMBL430371 1 7.96
CHEMBL239539 1 7.91
CHEMBL391895 1 7.82
CHEMBL240564 1 7.82
CHEMBL241659 1 7.75
CHEMBL241225 1 7.74
CHEMBL391120 1 7.64
CHEMBL241027 1 7.55
CHEMBL240378 1 7.55
CHEMBL391057 1 7.52
CHEMBL429462 1 7.52
CHEMBL392579 1 7.51
CHEMBL394189 1 7.49
CHEMBL401224 1 7.43
CHEMBL241660 1 7.41
CHEMBL401223 1 7.39
CHEMBL240587 1 7.37
CHEMBL240377 1 7.33
CHEMBL239065 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239923 Ki = 0.3 nM 9.52
CHEMBL25236 BP-897 Ki = 0.91 nM 9.04
CHEMBL241455 Ki = 2.4 nM 8.62
CHEMBL239706 Ki = 2.7 nM 8.57
CHEMBL394019 Ki = 2.82 nM 8.55
CHEMBL240600 Ki = 3.6 nM 8.44
CHEMBL239493 Ki = 6.01 nM 8.22
CHEMBL241026 Ki = 6.2 nM 8.21
CHEMBL240589 Ki = 8.72 nM 8.06
CHEMBL241226 Ki = 10.8 nM 7.97
CHEMBL430371 Ki = 10.9 nM 7.96
CHEMBL240588 Ki = 11.1 nM 7.96
CHEMBL239539 Ki = 12.3 nM 7.91
CHEMBL391895 Ki = 15.2 nM 7.82
CHEMBL240564 Ki = 15.2 nM 7.82
CHEMBL241659 Ki = 17.7 nM 7.75
CHEMBL241225 Ki = 18.4 nM 7.74
CHEMBL391120 Ki = 22.8 nM 7.64
CHEMBL241027 Ki = 28.4 nM 7.55
CHEMBL240378 Ki = 28.0 nM 7.55
CHEMBL429462 Ki = 30.2 nM 7.52
CHEMBL391057 Ki = 30.3 nM 7.52
CHEMBL392579 Ki = 31.1 nM 7.51
CHEMBL394189 Ki = 32.6 nM 7.49
CHEMBL401224 Ki = 36.9 nM 7.43
CHEMBL241660 Ki = 38.9 nM 7.41
CHEMBL401223 Ki = 40.9 nM 7.39
CHEMBL240587 Ki = 42.9 nM 7.37
CHEMBL240377 Ki = 47.3 nM 7.33
CHEMBL239065 Ki = 50.2 nM 7.30
CHEMBL393775 Ki = 99.1 nM 7.00
CHEMBL240379 Ki = 133.0 nM 6.88
CHEMBL436998 Ki = 340.0 nM 6.47
CHEMBL239066 Ki = 500.0 nM 6.30
CHEMBL238858 Ki = 500.0 nM 6.30
CHEMBL238875 Ki = 2340.0 nM 5.63
CHEMBL239067 Ki > 1000.0 nM -
CHEMBL239708 Ki > 1000.0 nM -
CHEMBL393774 Ki > 1000.0 nM -
CHEMBL238877 Ki > 1000.0 nM -
CHEMBL241018 Ki > 1000.0 nM -
CHEMBL392791 Ki > 1000.0 nM -
CHEMBL238859 Ki > 1000.0 nM -