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Assay Detail

CHEMBL829309

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

Binding
Inhibition of rat c-Jun N-terminal kinase 3
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mitogen-activated protein kinase 10 (CHEMBL4092)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.
Gaillard P, Jeanclaude-Etter I, Ardissone V, Arkinstall S, Cambet Y, Camps M, Chabert C, Church D, Cirillo R, Gretener D, Halazy S, Nichols A, Szyndralewiez C, Vitte PA, Gotteland JP.
J Med Chem (2005) 48 : 4596 -4607
PubMed 15999997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 6.13 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL363355 1 7.39
CHEMBL363254 1 7.19
CHEMBL372708 1 7.10
CHEMBL191581 1 7.10
CHEMBL1788116 1 6.92
CHEMBL371113 1 6.84
CHEMBL189841 1 6.83
CHEMBL364757 1 6.60
CHEMBL364637 1 6.60
CHEMBL363253 1 6.56
CHEMBL189852 1 6.47
CHEMBL190742 1 6.47
CHEMBL425902 1 6.46
CHEMBL189223 1 6.40
CHEMBL191376 1 6.39
CHEMBL365963 1 6.34
CHEMBL424815 1 6.33
CHEMBL191204 1 6.30
CHEMBL190597 1 6.29
CHEMBL370889 1 6.23
CHEMBL190250 1 6.22
CHEMBL364940 1 6.19
CHEMBL191465 1 6.18
CHEMBL191021 1 6.15
CHEMBL370899 1 6.12
CHEMBL191269 1 6.09
CHEMBL370477 1 6.02
CHEMBL363155 1 6.00
CHEMBL425553 1 5.89
CHEMBL370960 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL363355 IC50 = 41.0 nM 7.39
CHEMBL363254 IC50 = 65.0 nM 7.19
CHEMBL191581 IC50 = 80.0 nM 7.10
CHEMBL372708 IC50 = 80.0 nM 7.10
CHEMBL1788116 IC50 = 120.0 nM 6.92
CHEMBL371113 IC50 = 143.0 nM 6.84
CHEMBL189841 IC50 = 147.0 nM 6.83
CHEMBL364757 IC50 = 250.0 nM 6.60
CHEMBL364637 IC50 = 250.0 nM 6.60
CHEMBL363253 IC50 = 273.0 nM 6.56
CHEMBL189852 IC50 = 340.0 nM 6.47
CHEMBL190742 IC50 = 337.0 nM 6.47
CHEMBL425902 IC50 = 350.0 nM 6.46
CHEMBL189223 IC50 = 397.0 nM 6.40
CHEMBL191376 IC50 = 407.0 nM 6.39
CHEMBL365963 IC50 = 458.0 nM 6.34
CHEMBL424815 IC50 = 473.0 nM 6.33
CHEMBL191204 IC50 = 500.0 nM 6.30
CHEMBL190597 IC50 = 510.0 nM 6.29
CHEMBL370889 IC50 = 583.0 nM 6.23
CHEMBL190250 IC50 = 600.0 nM 6.22
CHEMBL364940 IC50 = 650.0 nM 6.19
CHEMBL191465 IC50 = 660.0 nM 6.18
CHEMBL191021 IC50 = 707.0 nM 6.15
CHEMBL370899 IC50 = 760.0 nM 6.12
CHEMBL191269 IC50 = 820.0 nM 6.09
CHEMBL370477 IC50 = 950.0 nM 6.02
CHEMBL363155 IC50 = 993.0 nM 6.00
CHEMBL425553 IC50 = 1300.0 nM 5.89
CHEMBL370960 IC50 = 1324.0 nM 5.88
CHEMBL191543 IC50 = 1340.0 nM 5.87
CHEMBL363556 IC50 = 1490.0 nM 5.83
CHEMBL190859 IC50 = 1644.0 nM 5.78
CHEMBL189421 IC50 = 1810.0 nM 5.74
CHEMBL188499 IC50 = 2900.0 nM 5.54
CHEMBL370516 IC50 = 3080.0 nM 5.51
CHEMBL373086 IC50 = 3500.0 nM 5.46
CHEMBL365191 IC50 = 3740.0 nM 5.43
CHEMBL364053 IC50 = 6500.0 nM 5.19
CHEMBL362934 IC50 = 6600.0 nM 5.18
CHEMBL365146 IC50 = 6800.0 nM 5.17
CHEMBL191536 IC50 = 7200.0 nM 5.14
CHEMBL190457 IC50 = 7500.0 nM 5.12
CHEMBL190380 IC50 = 9400.0 nM 5.03
CHEMBL189931 IC50 > 5000.0 nM -
CHEMBL189993 IC50 > 5000.0 nM -
CHEMBL190363 IC50 > 5000.0 nM -
CHEMBL362926 IC50 > 5000.0 nM -
CHEMBL372933 IC50 > 5000.0 nM -
CHEMBL191498 IC50 > 5000.0 nM -