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Assay Detail

CHEMBL4041968

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Binding
Inhibition of recombinant Leishmania donovani DYRK1B expressed in Escherichia coli using woodtide as substrate after 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting
ChEMBL ↗
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.
Bendjeddou LZ, Loaëc N, Villiers B, Prina E, Späth GF, Galons H, Meijer L, Oumata N.
Eur J Med Chem (2017) 125 : 696 -709
PubMed 27721154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 5.89 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4090770 — — 1 7.01
CHEMBL4061526 — — 1 6.96
CHEMBL4071322 — — 1 6.89
CHEMBL4082981 — — 1 6.89
CHEMBL4062820 — — 1 6.82
CHEMBL4105084 — — 1 6.72
CHEMBL4074132 — — 1 6.41
CHEMBL4065432 — — 1 6.39
CHEMBL4089652 — — 1 6.38
CHEMBL4104296 — — 1 6.38
CHEMBL4093104 — — 1 6.37
CHEMBL4070227 — — 1 6.32
CHEMBL1802358 — — 1 6.24
CHEMBL4074499 — — 1 6.23
CHEMBL4100956 — — 1 6.16
CHEMBL4102871 — — 1 6.16
CHEMBL4097368 — — 1 6.06
CHEMBL4072506 — — 1 6.01
CHEMBL4084919 — — 1 6.00
CHEMBL4086402 — — 1 5.92
CHEMBL4079347 — — 1 5.92
CHEMBL4070189 — — 1 5.80
CHEMBL4071013 — — 1 5.75
CHEMBL4091942 — — 1 5.75
CHEMBL4070065 — — 1 5.68
CHEMBL4092117 — — 1 5.68
CHEMBL4098107 — — 1 5.66
CHEMBL4092673 — — 1 5.66
CHEMBL4088717 — — 1 5.55
CHEMBL4063254 — — 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4090770 — IC50 = 98.0 nM 7.01
CHEMBL4061526 — IC50 = 110.0 nM 6.96
CHEMBL4082981 — IC50 = 130.0 nM 6.89
CHEMBL4071322 — IC50 = 130.0 nM 6.89
CHEMBL4062820 — IC50 = 150.0 nM 6.82
CHEMBL4105084 — IC50 = 190.0 nM 6.72
CHEMBL4074132 — IC50 = 390.0 nM 6.41
CHEMBL4065432 — IC50 = 410.0 nM 6.39
CHEMBL4089652 — IC50 = 420.0 nM 6.38
CHEMBL4104296 — IC50 = 420.0 nM 6.38
CHEMBL4093104 — IC50 = 430.0 nM 6.37
CHEMBL4070227 — IC50 = 480.0 nM 6.32
CHEMBL1802358 — IC50 = 580.0 nM 6.24
CHEMBL4074499 — IC50 = 590.0 nM 6.23
CHEMBL4102871 — IC50 = 690.0 nM 6.16
CHEMBL4100956 — IC50 = 690.0 nM 6.16
CHEMBL4097368 — IC50 = 880.0 nM 6.06
CHEMBL4072506 — IC50 = 980.0 nM 6.01
CHEMBL4084919 — IC50 = 1000.0 nM 6.00
CHEMBL4086402 — IC50 = 1200.0 nM 5.92
CHEMBL4079347 — IC50 = 1200.0 nM 5.92
CHEMBL4070189 — IC50 = 1600.0 nM 5.80
CHEMBL4071013 — IC50 = 1800.0 nM 5.75
CHEMBL4091942 — IC50 = 1800.0 nM 5.75
CHEMBL4092117 — IC50 = 2100.0 nM 5.68
CHEMBL4070065 — IC50 = 2100.0 nM 5.68
CHEMBL4098107 — IC50 = 2200.0 nM 5.66
CHEMBL4092673 — IC50 = 2200.0 nM 5.66
CHEMBL4088717 — IC50 = 2800.0 nM 5.55
CHEMBL4063254 — IC50 = 3100.0 nM 5.51
CHEMBL4090223 — IC50 = 3100.0 nM 5.51
CHEMBL4077159 — IC50 = 4100.0 nM 5.39
CHEMBL4071413 — IC50 = 4100.0 nM 5.39
CHEMBL4069158 — IC50 = 4100.0 nM 5.39
CHEMBL4084364 — IC50 = 6000.0 nM 5.22
CHEMBL4075820 — IC50 = 6100.0 nM 5.21
CHEMBL4061394 — IC50 = 6200.0 nM 5.21
CHEMBL4079343 — IC50 = 6900.0 nM 5.16
CHEMBL4076448 — IC50 = 7300.0 nM 5.14
CHEMBL4098237 — IC50 = 7900.0 nM 5.10
CHEMBL4093231 — IC50 = 8000.0 nM 5.10
CHEMBL4076663 — IC50 = 8100.0 nM 5.09
CHEMBL4089542 — IC50 = 8900.0 nM 5.05
CHEMBL4067420 — IC50 > 10000.0 nM -
CHEMBL4062683 — IC50 > 10000.0 nM -
CHEMBL4062568 — IC50 > 10000.0 nM -
CHEMBL4077125 — IC50 > 10000.0 nM -
CHEMBL4091127 — IC50 > 10000.0 nM -
CHEMBL4064988 — IC50 > 10000.0 nM -
CHEMBL4075509 — IC50 > 10000.0 nM -