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Assay Detail

CHEMBL2214786

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Binding
Inhibition of JAK3
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK3 (CHEMBL2148)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P.
Bioorg Med Chem Lett (2012) 22 : 7653 -7658
PubMed 23127890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.45 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2208035 1 7.21
CHEMBL2208028 1 6.98
CHEMBL2208033 1 6.80
CHEMBL2208034 1 6.67
CHEMBL2208031 1 6.53
CHEMBL2208032 1 6.51
CHEMBL2207758 1 6.43
CHEMBL2207759 1 6.32
CHEMBL2207760 1 6.25
CHEMBL2208023 1 5.94
CHEMBL2207763 1 5.30
CHEMBL2208030 1 -
CHEMBL2208029 1 -
CHEMBL2208027 1 -
CHEMBL2208026 1 -
CHEMBL1077458 1 -
CHEMBL2208025 1 -
CHEMBL2208024 1 -
CHEMBL2207767 1 -
CHEMBL2207766 1 -
CHEMBL2207765 1 -
CHEMBL2207764 1 -
CHEMBL2207761 1 -
CHEMBL2207762 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2208035 IC50 = 61.7 nM 7.21
CHEMBL2208028 IC50 = 104.5 nM 6.98
CHEMBL2208033 IC50 = 159.8 nM 6.80
CHEMBL2208034 IC50 = 214.2 nM 6.67
CHEMBL2208031 IC50 = 298.3 nM 6.53
CHEMBL2208032 IC50 = 306.8 nM 6.51
CHEMBL2207758 IC50 = 368.1 nM 6.43
CHEMBL2207759 IC50 = 483.8 nM 6.32
CHEMBL2207760 IC50 = 557.3 nM 6.25
CHEMBL2208023 IC50 = 1149.3 nM 5.94
CHEMBL2207763 IC50 = 5000.0 nM 5.30
CHEMBL2208030 IC50 > 980.0 nM -
CHEMBL2208029 IC50 > 980.0 nM -
CHEMBL2208027 IC50 > 980.0 nM -
CHEMBL2208026 IC50 > 980.0 nM -
CHEMBL1077458 IC50 > 980.0 nM -
CHEMBL2208025 IC50 > 980.0 nM -
CHEMBL2208024 IC50 > 980.0 nM -
CHEMBL2207767 IC50 > 980.0 nM -
CHEMBL2207766 IC50 > 980.0 nM -
CHEMBL2207765 IC50 > 980.0 nM -
CHEMBL2207764 IC50 > 980.0 nM -
CHEMBL2207761 IC50 > 5000.0 nM -
CHEMBL2207762 IC50 > 980.0 nM -