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Assay Detail

CHEMBL3424258

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Binding
Inhibition of Leishmania CRK3/CYC6 using histone H1/[gamma33-P]ATP as substrate after 30 mins
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Leishmania
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro.
Řezníčková E, Popa A, Gucký T, Zatloukal M, Havlíček L, Bazgier V, Berka K, Jorda R, Popa I, Nasereddin A, Jaffe CL, Kryštof V, Strnad M.
Bioorg Med Chem Lett (2015) 25 : 2298 -2301
PubMed 25937014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.44 6.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3423087 1 6.94
CHEMBL3423080 1 6.79
CHEMBL3423086 1 6.67
CHEMBL3423075 1 6.50
CHEMBL3423076 1 6.42
CHEMBL1094304 OLOMOUCINE II 1 6.23
CHEMBL2349189 1 6.19
CHEMBL3423079 1 5.78
CHEMBL3423090 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3423087 IC50 = 115.0 nM 6.94
CHEMBL3423080 IC50 = 162.0 nM 6.79
CHEMBL3423086 IC50 = 214.0 nM 6.67
CHEMBL3423075 IC50 = 314.0 nM 6.50
CHEMBL3423076 IC50 = 384.0 nM 6.42
CHEMBL1094304 OLOMOUCINE II IC50 = 590.0 nM 6.23
CHEMBL2349189 IC50 = 641.0 nM 6.19
CHEMBL3423079 IC50 = 1648.0 nM 5.78
CHEMBL3423090 IC50 - -