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Assay Detail

CHEMBL1045264

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Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

P2Y purinoceptor 14 (CHEMBL4518)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Human P2Y(14) receptor agonists: truncation of the hexose moiety of uridine-5'-diphosphoglucose and its replacement with alkyl and aryl groups.
Das A, Ko H, Burianek LE, Barrett MO, Harden TK, Jacobson KA.
J Med Chem (2010) 53 : 471 -480
PubMed 19902968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 6.69 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL611791 1 9.04
CHEMBL216011 1 8.72
CHEMBL374384 1 7.96
CHEMBL611792 1 7.96
CHEMBL507060 1 7.96
CHEMBL1162556 1 7.50
CHEMBL1162563 1 7.41
CHEMBL1162553 1 7.40
CHEMBL1162557 1 7.25
CHEMBL488133 1 7.20
CHEMBL566925 1 6.85
CHEMBL130266 URIDINE_DIPHOSPHATE 1 6.80
CHEMBL612065 1 6.78
CHEMBL1162552 1 6.60
CHEMBL384992 1 6.50
CHEMBL375951 URIDINE DIPHOSPHATE GLUCOSE 1 6.40
CHEMBL612064 1 6.32
CHEMBL1162559 1 6.12
CHEMBL612119 1 5.83
CHEMBL1162560 1 5.80
CHEMBL1162561 1 5.75
CHEMBL1162562 1 5.72
CHEMBL1162554 1 5.56
CHEMBL1204010 1 5.48
CHEMBL612063 1 5.34
CHEMBL1162558 1 5.29
CHEMBL1162555 1 5.13
CHEMBL608851 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL611791 EC50 = 0.92 nM 9.04
CHEMBL216011 EC50 = 1.92 nM 8.72
CHEMBL374384 EC50 = 11.0 nM 7.96
CHEMBL611792 EC50 = 11.0 nM 7.96
CHEMBL507060 EC50 = 11.0 nM 7.96
CHEMBL1162556 EC50 = 32.0 nM 7.50
CHEMBL1162563 EC50 = 39.0 nM 7.41
CHEMBL1162553 EC50 = 40.0 nM 7.40
CHEMBL1162557 EC50 = 56.0 nM 7.25
CHEMBL488133 EC50 = 63.0 nM 7.20
CHEMBL566925 EC50 = 142.0 nM 6.85
CHEMBL130266 URIDINE_DIPHOSPHATE EC50 = 160.0 nM 6.80
CHEMBL612065 EC50 = 167.0 nM 6.78
CHEMBL1162552 EC50 = 252.0 nM 6.60
CHEMBL384992 EC50 = 320.0 nM 6.50
CHEMBL375951 URIDINE DIPHOSPHATE GLUCOSE EC50 = 400.0 nM 6.40
CHEMBL612064 EC50 = 480.0 nM 6.32
CHEMBL1162559 EC50 = 768.0 nM 6.12
CHEMBL612119 EC50 = 1490.0 nM 5.83
CHEMBL1162560 EC50 = 1600.0 nM 5.80
CHEMBL1162561 EC50 = 1800.0 nM 5.75
CHEMBL1162562 EC50 = 1900.0 nM 5.72
CHEMBL1162554 EC50 = 2730.0 nM 5.56
CHEMBL1204010 EC50 = 3320.0 nM 5.48
CHEMBL612063 EC50 = 4580.0 nM 5.34
CHEMBL1162558 EC50 = 5160.0 nM 5.29
CHEMBL1162555 EC50 = 7460.0 nM 5.13
CHEMBL608851 EC50 - -