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Assay Detail

CHEMBL4369944

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Binding
Inhibition of sigma receptor 1 (unknown origin)
8
Total Activities
8
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

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and in Vivo Characterization of A<sub>1</sub> Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series.
Tosh DK, Rao H, Bitant A, Salmaso V, Mannes P, Lieberman DI, Vaughan KL, Mattison JA, Rothwell AC, Auchampach JA, Ciancetta A, Liu N, Cui Z, Gao ZG, Reitman ML, Gavrilova O, Jacobson KA.
J Med Chem (2019) 62 : 1502 -1522
PubMed 30605331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.89 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4541086 1 6.32
CHEMBL4436917 1 6.20
CHEMBL4439013 1 6.16
CHEMBL595547 5'-CARBOXY ADENOSINE 1 5.83
CHEMBL4554295 1 5.82
CHEMBL4436786 1 5.75
CHEMBL4543137 1 5.71
CHEMBL2170801 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4541086 Ki = 484.0 nM 6.32
CHEMBL4436917 Ki = 626.0 nM 6.20
CHEMBL4439013 Ki = 690.0 nM 6.16
CHEMBL595547 5'-CARBOXY ADENOSINE Ki = 1480.0 nM 5.83
CHEMBL4554295 Ki = 1500.0 nM 5.82
CHEMBL4436786 Ki = 1790.0 nM 5.75
CHEMBL4543137 Ki = 1970.0 nM 5.71
CHEMBL2170801 Ki = 5090.0 nM 5.29