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Assay Detail

CHEMBL3243862

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Binding
Inhibition of adrenergic alpha1B receptor (unknown origin)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Li P, Zhang Q, Robichaud AJ, Lee T, Tomesch J, Yao W, Beard JD, Snyder GL, Zhu H, Peng Y, Hendrick JP, Vanover KE, Davis RE, Mates S, Wennogle LP.
J Med Chem (2014) 57 : 2670 -2682
PubMed 24559051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.05 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233142 LUMATEPERONE TOSYLATE 4.0 1 7.51
CHEMBL3233412 1 7.18
CHEMBL3233432 1 6.98
CHEMBL3233411 1 6.53
CHEMBL3233143 1 -
CHEMBL3233427 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233142 LUMATEPERONE TOSYLATE Ki = 31.0 nM 7.51
CHEMBL3233412 Ki = 66.0 nM 7.18
CHEMBL3233432 Ki = 104.0 nM 6.98
CHEMBL3233411 Ki = 294.0 nM 6.53
CHEMBL3233143 Ki - -
CHEMBL3233427 Ki - -