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Assay Detail

CHEMBL833177

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Functional
Concentration required for calcium mobilization at rat purinergic 2Y1 receptor expressed in HEK 293 cells
12
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

P2Y purinoceptor 1 (CHEMBL2497)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Molecular recognition in purinergic receptors. 2. Diastereoselectivity of the h-P2Y1-receptor.
Major DT, Nahum V, Wang Y, Reiser G, Fischer B.
J Med Chem (2004) 47 : 4405 -4416
PubMed 15317453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.77 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336208 1 9.00
CHEMBL2093075 1 9.00
CHEMBL2364572 2 8.59
CHEMBL610595 2 8.35
CHEMBL2093074 1 8.03
CHEMBL2092819 1 7.70
CHEMBL2092818 1 7.12
CHEMBL611086 2 6.70
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336208 EC50 = 1.0 nM 9.00
CHEMBL2093075 EC50 = 1.0 nM 9.00
CHEMBL2364572 EC50 = 2.6 nM 8.59
CHEMBL610595 EC50 = 4.5 nM 8.35
CHEMBL2093074 EC50 = 9.4 nM 8.03
CHEMBL2092819 EC50 = 20.0 nM 7.70
CHEMBL610595 EC50 = 36.0 nM 7.44
CHEMBL2364572 EC50 = 53.0 nM 7.28
CHEMBL2092818 EC50 = 75.0 nM 7.12
CHEMBL611086 EC50 = 200.0 nM 6.70
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 590.0 nM 6.23
CHEMBL611086 EC50 > 1000.0 nM -