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Assay Detail

CHEMBL908418

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Binding
Inhibition of JAK2
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of pyrimidine-based inhibitors of Janus tyrosine kinase 3.
Chen JJ, Thakur KD, Clark MP, Laughlin SK, George KM, Bookland RG, Davis JR, Cabrera EJ, Easwaran V, De B, George Zhang Y.
Bioorg Med Chem Lett (2006) 16 : 5633 -5638
PubMed 16934457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.30 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL221029 1 8.40
CHEMBL218579 1 8.15
CHEMBL221976 1 8.10
CHEMBL221959 TOFACITINIB 4.0 1 7.96
CHEMBL220483 1 7.92
CHEMBL222027 1 7.80
CHEMBL218439 1 7.77
CHEMBL374321 1 7.75
CHEMBL375296 1 7.72
CHEMBL384820 1 7.70
CHEMBL221378 1 7.55
CHEMBL375205 1 7.54
CHEMBL375076 1 7.31
CHEMBL218746 1 7.29
CHEMBL220585 1 7.29
CHEMBL220969 1 7.25
CHEMBL221037 1 7.23
CHEMBL385114 1 7.17
CHEMBL221376 1 7.11
CHEMBL376885 1 6.95
CHEMBL221912 1 6.91
CHEMBL557844 1 6.85
CHEMBL218602 1 6.82
CHEMBL373523 1 6.78
CHEMBL220484 1 6.35
CHEMBL323994 1 6.22
CHEMBL221038 1 5.14
CHEMBL222028 1 -
CHEMBL374854 1 -
CHEMBL217937 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL221029 IC50 = 4.0 nM 8.40
CHEMBL218579 IC50 = 7.0 nM 8.15
CHEMBL221976 IC50 = 8.0 nM 8.10
CHEMBL221959 TOFACITINIB IC50 = 11.0 nM 7.96
CHEMBL220483 IC50 = 12.0 nM 7.92
CHEMBL222027 IC50 = 16.0 nM 7.80
CHEMBL218439 IC50 = 17.0 nM 7.77
CHEMBL374321 IC50 = 18.0 nM 7.75
CHEMBL375296 IC50 = 19.0 nM 7.72
CHEMBL384820 IC50 = 20.0 nM 7.70
CHEMBL221378 IC50 = 28.0 nM 7.55
CHEMBL375205 IC50 = 29.0 nM 7.54
CHEMBL375076 IC50 = 49.0 nM 7.31
CHEMBL218746 IC50 = 51.0 nM 7.29
CHEMBL220585 IC50 = 51.0 nM 7.29
CHEMBL220969 IC50 = 56.0 nM 7.25
CHEMBL221037 IC50 = 59.0 nM 7.23
CHEMBL385114 IC50 = 68.0 nM 7.17
CHEMBL221376 IC50 = 77.0 nM 7.11
CHEMBL376885 IC50 = 113.0 nM 6.95
CHEMBL221912 IC50 = 124.0 nM 6.91
CHEMBL557844 IC50 = 141.0 nM 6.85
CHEMBL218602 IC50 = 153.0 nM 6.82
CHEMBL373523 IC50 = 167.0 nM 6.78
CHEMBL220484 IC50 = 446.0 nM 6.35
CHEMBL323994 IC50 = 600.0 nM 6.22
CHEMBL221038 IC50 = 7218.0 nM 5.14
CHEMBL222028 IC50 > 10000.0 nM -
CHEMBL374854 IC50 > 10000.0 nM -
CHEMBL217937 IC50 > 10000.0 nM -