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Assay Detail

CHEMBL944826

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

Binding
Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Fibroblast
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1-Aminoindanes as novel motif with potential atypical antipsychotic properties.
Graham JM, Coughenour LL, Barr BM, Rock DL, Nikam SS.
Bioorg Med Chem Lett (2008) 18 : 489 -493
PubMed 18160289 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.57 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL398711 1 9.52
CHEMBL252031 1 9.35
CHEMBL398525 1 9.31
CHEMBL708 ZIPRASIDONE 4.0 1 9.30
CHEMBL252230 1 9.14
CHEMBL252228 1 9.05
CHEMBL252818 1 8.87
CHEMBL398744 1 8.86
CHEMBL251834 1 8.73
CHEMBL252816 1 8.72
CHEMBL253024 1 8.65
CHEMBL404000 1 8.56
CHEMBL253022 1 8.52
CHEMBL252030 1 8.50
CHEMBL398619 1 8.48
CHEMBL400236 1 8.44
CHEMBL400235 1 8.40
CHEMBL253878 1 8.28
CHEMBL253439 1 8.25
CHEMBL442290 1 7.99
CHEMBL252201 1 7.99
CHEMBL253233 1 7.96
CHEMBL398618 1 7.87
CHEMBL252429 1 7.81
CHEMBL252430 1 7.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398711 Ki = 0.3 nM 9.52
CHEMBL252031 Ki = 0.45 nM 9.35
CHEMBL398525 Ki = 0.49 nM 9.31
CHEMBL708 ZIPRASIDONE Ki = 0.5 nM 9.30
CHEMBL252230 Ki = 0.73 nM 9.14
CHEMBL252228 Ki = 0.9 nM 9.05
CHEMBL252818 Ki = 1.34 nM 8.87
CHEMBL398744 Ki = 1.38 nM 8.86
CHEMBL251834 Ki = 1.88 nM 8.73
CHEMBL252816 Ki = 1.92 nM 8.72
CHEMBL253024 Ki = 2.22 nM 8.65
CHEMBL404000 Ki = 2.72 nM 8.56
CHEMBL253022 Ki = 3.03 nM 8.52
CHEMBL252030 Ki = 3.18 nM 8.50
CHEMBL398619 Ki = 3.31 nM 8.48
CHEMBL400236 Ki = 3.61 nM 8.44
CHEMBL400235 Ki = 3.96 nM 8.40
CHEMBL253878 Ki = 5.27 nM 8.28
CHEMBL253439 Ki = 5.64 nM 8.25
CHEMBL442290 Ki = 10.26 nM 7.99
CHEMBL252201 Ki = 10.33 nM 7.99
CHEMBL253233 Ki = 10.91 nM 7.96
CHEMBL398618 Ki = 13.54 nM 7.87
CHEMBL252429 Ki = 15.58 nM 7.81
CHEMBL252430 Ki = 17.37 nM 7.76