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Assay Detail

CHEMBL5153128

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
50
Total Activities
50
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 Autocuration

Target

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

Publication

Discovery of a Series of 5-Amide-1<i>H</i>-pyrazole-3-carboxyl Derivatives as Potent P2Y<sub>14</sub>R Antagonists with Anti-Inflammatory Characters.
Wang YH, Zhou MZ, Ye T, Wang PP, Lu R, Wang YL, Liu CX, Xiao W, Li JY, Meng ZB, Xu LL, Hu QH, Jiang C.
J Med Chem (2022) 65 : 15967 -15990
PubMed 36394994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 7.69 8.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208130 1 8.71
CHEMBL1800685 PPTN 1 8.70
CHEMBL5203559 1 8.42
CHEMBL5194881 1 8.42
CHEMBL5182459 1 8.40
CHEMBL5175291 1 8.38
CHEMBL5189241 1 8.33
CHEMBL5192153 1 8.33
CHEMBL5185002 1 8.32
CHEMBL5195243 1 8.30
CHEMBL5203936 1 8.27
CHEMBL5182261 1 8.24
CHEMBL5208342 1 8.15
CHEMBL5169372 1 7.85
CHEMBL5183974 1 7.80
CHEMBL5205552 1 7.39
CHEMBL5203764 1 7.21
CHEMBL5188038 1 7.17
CHEMBL5209515 1 7.00
CHEMBL5181115 1 6.96
CHEMBL5189945 1 6.87
CHEMBL5170216 1 6.77
CHEMBL5189099 1 6.64
CHEMBL5194765 1 6.61
CHEMBL5206480 1 6.43
CHEMBL5205688 1 6.27
CHEMBL5183561 1 -
CHEMBL5209203 1 -
CHEMBL5184856 1 -
CHEMBL5187389 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208130 IC50 = 1.93 nM 8.71
CHEMBL1800685 PPTN IC50 = 1.98 nM 8.70
CHEMBL5194881 IC50 = 3.83 nM 8.42
CHEMBL5203559 IC50 = 3.81 nM 8.42
CHEMBL5182459 IC50 = 4.01 nM 8.40
CHEMBL5175291 IC50 = 4.16 nM 8.38
CHEMBL5189241 IC50 = 4.65 nM 8.33
CHEMBL5192153 IC50 = 4.66 nM 8.33
CHEMBL5185002 IC50 = 4.83 nM 8.32
CHEMBL5195243 IC50 = 5.0 nM 8.30
CHEMBL5203936 IC50 = 5.39 nM 8.27
CHEMBL5182261 IC50 = 5.77 nM 8.24
CHEMBL5208342 IC50 = 7.11 nM 8.15
CHEMBL5169372 IC50 = 14.26 nM 7.85
CHEMBL5183974 IC50 = 15.7 nM 7.80
CHEMBL5205552 IC50 = 40.95 nM 7.39
CHEMBL5203764 IC50 = 61.22 nM 7.21
CHEMBL5188038 IC50 = 67.0 nM 7.17
CHEMBL5209515 IC50 = 99.65 nM 7.00
CHEMBL5181115 IC50 = 110.9 nM 6.96
CHEMBL5189945 IC50 = 135.7 nM 6.87
CHEMBL5170216 IC50 = 170.8 nM 6.77
CHEMBL5189099 IC50 = 227.3 nM 6.64
CHEMBL5194765 IC50 = 245.1 nM 6.61
CHEMBL5206480 IC50 = 369.0 nM 6.43
CHEMBL5205688 IC50 = 531.5 nM 6.27
CHEMBL5199447 IC50 - -
CHEMBL5208928 IC50 - -
CHEMBL5187483 IC50 - -
CHEMBL5201558 IC50 - -
CHEMBL5192477 IC50 - -
CHEMBL5203691 IC50 - -
CHEMBL5188554 IC50 - -
CHEMBL5204691 IC50 - -
CHEMBL5175975 IC50 - -
CHEMBL5173350 IC50 - -
CHEMBL5181431 IC50 - -
CHEMBL5173736 IC50 - -
CHEMBL5183561 IC50 - -
CHEMBL5183434 IC50 - -
CHEMBL5178378 IC50 - -
CHEMBL5171287 IC50 - -
CHEMBL5185373 IC50 - -
CHEMBL5205395 IC50 - -
CHEMBL5182974 IC50 - -
CHEMBL5208178 IC50 - -
CHEMBL5194585 IC50 - -
CHEMBL5187389 IC50 - -
CHEMBL5184856 IC50 - -
CHEMBL5209203 IC50 - -