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Assay Detail

CHEMBL760442

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

Functional
Inhibition of PAF-induced platelet aggregation
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Platelet-activating factor receptor (CHEMBL5136)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and structure-activity relationships of 1-acyl-4-((2-methyl-3-pyridyl)cyanomethyl)piperazines as PAF antagonists.
Carceller E, Merlos M, Giral M, Almansa C, Bartrolí J, García-Rafanell J, Forn J.
J Med Chem (1993) 36 : 2984 -2997
PubMed 8411016 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 7.36 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL102070 1 8.05
CHEMBL100497 1 8.04
CHEMBL322184 1 8.04
CHEMBL102918 1 8.04
CHEMBL103596 1 7.96
CHEMBL103393 1 7.92
CHEMBL103476 1 7.89
CHEMBL318563 1 7.85
CHEMBL420092 1 7.80
CHEMBL100641 1 7.77
CHEMBL100642 1 7.75
CHEMBL103995 1 7.75
CHEMBL100809 1 7.70
CHEMBL100340 1 7.70
CHEMBL319229 1 7.70
CHEMBL101245 1 7.70
CHEMBL431049 1 7.66
CHEMBL103903 1 7.58
CHEMBL103560 1 7.58
CHEMBL100547 1 7.55
CHEMBL103408 1 7.52
CHEMBL103571 1 7.52
CHEMBL100190 1 7.52
CHEMBL102774 1 7.51
CHEMBL99795 1 7.47
CHEMBL103368 1 7.44
CHEMBL103773 1 7.42
CHEMBL100493 1 7.40
CHEMBL418792 1 7.39
CHEMBL103761 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL102070 IC50 = 8.9 nM 8.05
CHEMBL100497 IC50 = 9.1 nM 8.04
CHEMBL102918 IC50 = 9.1 nM 8.04
CHEMBL322184 IC50 = 9.1 nM 8.04
CHEMBL103596 IC50 = 11.0 nM 7.96
CHEMBL103393 IC50 = 12.0 nM 7.92
CHEMBL103476 IC50 = 13.0 nM 7.89
CHEMBL318563 IC50 = 14.0 nM 7.85
CHEMBL420092 IC50 = 16.0 nM 7.80
CHEMBL100641 IC50 = 17.0 nM 7.77
CHEMBL100642 IC50 = 18.0 nM 7.75
CHEMBL103995 IC50 = 18.0 nM 7.75
CHEMBL100340 IC50 = 20.0 nM 7.70
CHEMBL100809 IC50 = 20.0 nM 7.70
CHEMBL319229 IC50 = 20.0 nM 7.70
CHEMBL101245 IC50 = 20.0 nM 7.70
CHEMBL431049 IC50 = 22.0 nM 7.66
CHEMBL103903 IC50 = 26.0 nM 7.58
CHEMBL103560 IC50 = 26.0 nM 7.58
CHEMBL100547 IC50 = 28.0 nM 7.55
CHEMBL103408 IC50 = 30.0 nM 7.52
CHEMBL103571 IC50 = 30.0 nM 7.52
CHEMBL100190 IC50 = 30.0 nM 7.52
CHEMBL102774 IC50 = 31.0 nM 7.51
CHEMBL99795 IC50 = 34.0 nM 7.47
CHEMBL103368 IC50 = 36.0 nM 7.44
CHEMBL103773 IC50 = 38.0 nM 7.42
CHEMBL100493 IC50 = 40.0 nM 7.40
CHEMBL418792 IC50 = 41.0 nM 7.39
CHEMBL103761 IC50 = 41.0 nM 7.39
CHEMBL103180 IC50 = 42.0 nM 7.38
CHEMBL273945 IC50 = 50.0 nM 7.30
CHEMBL103801 IC50 = 53.0 nM 7.28
CHEMBL102666 IC50 = 56.0 nM 7.25
CHEMBL318163 IC50 = 63.0 nM 7.20
CHEMBL100971 IC50 = 64.0 nM 7.19
CHEMBL103171 IC50 = 68.0 nM 7.17
CHEMBL319960 IC50 = 75.0 nM 7.12
CHEMBL318159 IC50 = 80.0 nM 7.10
CHEMBL103477 IC50 = 79.0 nM 7.10
CHEMBL103561 IC50 = 86.0 nM 7.07
CHEMBL280164 APAFANT IC50 = 91.0 nM 7.04
CHEMBL100597 IC50 = 120.0 nM 6.92
CHEMBL318460 IC50 = 150.0 nM 6.82
CHEMBL320676 IC50 = 270.0 nM 6.57
CHEMBL421204 IC50 = 470.0 nM 6.33
CHEMBL100853 IC50 = 740.0 nM 6.13
CHEMBL101957 IC50 = 860.0 nM 6.07
CHEMBL103546 IC50 = 15200.0 nM 4.82