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Assay Detail

CHEMBL3888134

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

Binding
Cellular Proliferation Assay: Test compounds were resuspended in DMSO at a concentration of 10 mM. A serial three-fold dilution of each compound with DMSO was performed in 384-well plates using the Janus Liquid Dispenser (PerkinElmer). Compound was delivered to the assay plates containing 2500 cells in a 50 μL volume via Acoustic delivery from an ATS-100 (EDC). For Ba/F3-BCR-ABL1-WT cell assays, 2 nL of each compound dilution was transferred to the assay plate for final assay concentrations of 0.4 μM, 0.13 μM, 0.044 μM, 0.015 μM, 0.005 μM, 0.001 μM, 0.00033 μM, 0.00011 μM, 0.000037 μM, 0.000012 μM. For Ba/F3-WT and Ba/F3-BCR-ABL1-T315I cell assays, 50 nL of each compound dilution was transferred to the assay plate for final assay concentrations of 10 μM, 3.33 μM, 1.11 μM, 0.37 μM, 0.12 μM, 0.041 μM, 0.014 μM, 0.0046 μM, 0.0015 μM, 0.00051 μM.Cells were incubated at 37° C. in a humidified environment with 5% car
ChEMBL ↗
56
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase ABL1 (CHEMBL1862) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Compounds and compositions for inhibiting the activity of ABL1, ABL2 and BCR-ABL1
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 7.67 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4110570 — — 2 9.30
CHEMBL4106838 — — 2 9.30
CHEMBL4106732 — — 2 9.15
CHEMBL4113224 — — 2 9.10
CHEMBL4106602 — — 2 9.05
CHEMBL4108652 — — 2 9.05
CHEMBL3943799 — — 2 8.96
CHEMBL3953095 — — 2 8.89
CHEMBL3937525 — — 2 8.85
CHEMBL4107033 — — 2 8.66
CHEMBL4110566 — — 2 8.62
CHEMBL4115154 — — 2 8.54
CHEMBL3901435 — — 2 8.49
CHEMBL4107401 — — 2 8.41
CHEMBL3942231 — — 2 8.31
CHEMBL3906709 — — 2 8.28
CHEMBL4109149 — — 2 8.25
CHEMBL4114324 — — 2 8.18
CHEMBL5767231 — — 2 8.13
CHEMBL3898258 — — 2 8.05
CHEMBL3903302 — — 2 8.05
CHEMBL3986284 — — 2 7.99
CHEMBL4109872 — — 2 7.90
CHEMBL3951459 — — 2 7.89
CHEMBL3897706 — — 2 7.67
CHEMBL4108925 — — 2 7.61
CHEMBL4110478 — — 2 7.36
CHEMBL4113196 — — 2 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4110570 — IC50 = 0.5 nM 9.30
CHEMBL4106838 — IC50 = 0.5 nM 9.30
CHEMBL4106732 — IC50 = 0.7 nM 9.15
CHEMBL4113224 — IC50 = 0.8 nM 9.10
CHEMBL4106602 — IC50 = 0.9 nM 9.05
CHEMBL4108652 — IC50 = 0.9 nM 9.05
CHEMBL3943799 — IC50 = 1.1 nM 8.96
CHEMBL3953095 — IC50 = 1.3 nM 8.89
CHEMBL3937525 — IC50 = 1.4 nM 8.85
CHEMBL4107033 — IC50 = 2.2 nM 8.66
CHEMBL4110566 — IC50 = 2.4 nM 8.62
CHEMBL4115154 — IC50 = 2.9 nM 8.54
CHEMBL3901435 — IC50 = 3.2 nM 8.49
CHEMBL4107401 — IC50 = 3.9 nM 8.41
CHEMBL3942231 — IC50 = 4.9 nM 8.31
CHEMBL3906709 — IC50 = 5.3 nM 8.28
CHEMBL4109149 — IC50 = 5.6 nM 8.25
CHEMBL4114324 — IC50 = 6.6 nM 8.18
CHEMBL5767231 — IC50 = 7.4 nM 8.13
CHEMBL3898258 — IC50 = 9.0 nM 8.05
CHEMBL3903302 — IC50 = 8.9 nM 8.05
CHEMBL4106602 — IC50 = 10.0 nM 8.00
CHEMBL3986284 — IC50 = 10.2 nM 7.99
CHEMBL4106838 — IC50 = 12.0 nM 7.92
CHEMBL4109872 — IC50 = 12.5 nM 7.90
CHEMBL4110570 — IC50 = 13.0 nM 7.89
CHEMBL3951459 — IC50 = 12.9 nM 7.89
CHEMBL4106732 — IC50 = 19.0 nM 7.72
CHEMBL3897706 — IC50 = 21.6 nM 7.67
CHEMBL4108652 — IC50 = 24.0 nM 7.62
CHEMBL4113224 — IC50 = 24.0 nM 7.62
CHEMBL4108925 — IC50 = 24.6 nM 7.61
CHEMBL3953095 — IC50 = 35.0 nM 7.46
CHEMBL4107033 — IC50 = 36.0 nM 7.44
CHEMBL3937525 — IC50 = 38.0 nM 7.42
CHEMBL3943799 — IC50 = 38.0 nM 7.42
CHEMBL4110478 — IC50 = 43.5 nM 7.36
CHEMBL4113196 — IC50 = 47.0 nM 7.33
CHEMBL4115154 — IC50 = 88.0 nM 7.06
CHEMBL3901435 — IC50 = 93.0 nM 7.03
CHEMBL4110566 — IC50 = 124.0 nM 6.91
CHEMBL4107401 — IC50 = 130.0 nM 6.89
CHEMBL3942231 — IC50 = 130.0 nM 6.89
CHEMBL3906709 — IC50 = 165.0 nM 6.78
CHEMBL5767231 — IC50 = 169.0 nM 6.77
CHEMBL3898258 — IC50 = 213.0 nM 6.67
CHEMBL3951459 — IC50 = 273.0 nM 6.56
CHEMBL3897706 — IC50 = 370.0 nM 6.43
CHEMBL4113196 — IC50 = 442.0 nM 6.36
CHEMBL3986284 — IC50 = 513.0 nM 6.29