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Assay Detail

CHEMBL4370000

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Functional
Agonist activity at rat A1A adenosine receptor expressed in CHO-K1 cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
EC50 2 8.48 8.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284969 1 8.78
CHEMBL2012686 1 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284969 EC50 = 1.65 nM 8.78
CHEMBL2012686 EC50 = 6.65 nM 8.18