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Assay Detail

CHEMBL1948475

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

Binding
Displacement of [3H]prazosin from human recombinant alpha1B adrenoceptor expressed in CHO cells after 30 mins by liquid scintillation counting
17
Total Activities
17
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 Autocuration

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors.
Prandi A, Franchini S, Manasieva LI, Fossa P, Cichero E, Marucci G, Buccioni M, Cilia A, Pirona L, Brasili L.
J Med Chem (2012) 55 : 23 -36
PubMed 22145629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.10 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946777 1 8.17
CHEMBL1946780 1 8.05
CHEMBL1946779 1 7.40
CHEMBL286003 1 7.33
CHEMBL37883 1 7.20
CHEMBL514874 1 7.18
CHEMBL1946786 1 7.13
CHEMBL1946778 1 6.91
CHEMBL1946783 1 6.85
CHEMBL1946787 1 6.78
CHEMBL1946788 1 6.61
CHEMBL1946785 1 6.54
CHEMBL13647 BMY-7378 1 6.15
CHEMBL1946781 1 -
CHEMBL1946782 1 -
CHEMBL1946784 1 -
CHEMBL56 8-OH-DPAT 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946777 Ki = 6.761 nM 8.17
CHEMBL1946780 Ki = 8.913 nM 8.05
CHEMBL1946779 Ki = 39.81 nM 7.40
CHEMBL286003 Ki = 46.77 nM 7.33
CHEMBL37883 Ki = 63.1 nM 7.20
CHEMBL514874 Ki = 66.07 nM 7.18
CHEMBL1946786 Ki = 74.13 nM 7.13
CHEMBL1946778 Ki = 123.03 nM 6.91
CHEMBL1946783 Ki = 141.25 nM 6.85
CHEMBL1946787 Ki = 165.96 nM 6.78
CHEMBL1946788 Ki = 245.47 nM 6.61
CHEMBL1946785 Ki = 288.4 nM 6.54
CHEMBL13647 BMY-7378 Ki = 707.95 nM 6.15
CHEMBL1946781 Ki > 1000.0 nM -
CHEMBL1946782 Ki > 1000.0 nM -
CHEMBL1946784 Ki > 1000.0 nM -
CHEMBL56 8-OH-DPAT Ki > 1000.0 nM -