Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3887074

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

Binding
Inhibition Assay: ALK-inhibiting activity was measured by following an activity of inhibiting phosphorylation by biotinylated peptide (EGPWLEEEEEAYGWMDF). For the detection of phosphorylation of the biotinylated peptide, time-resolved fluorescence measurement was performed using an anti-phosphorylated tyrosine antibody labeled with europium cryptate and streptavidin conjugated to XL665, i.e., an allophycocyanin derivative.
ChEMBL ↗
266
Total Activities
262
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

ALK tyrosine kinase receptor (CHEMBL4247) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetracyclic compound
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 266 7.30 9.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3892880 — — 1 9.78
CHEMBL3917178 — — 1 9.52
CHEMBL3953815 — — 1 9.52
CHEMBL3929615 — — 1 9.52
CHEMBL3946496 — — 1 9.49
CHEMBL3915577 — — 1 9.49
CHEMBL3944715 — — 1 9.41
CHEMBL3936548 — — 1 9.40
CHEMBL3986700 — — 1 9.40
CHEMBL3938280 — — 1 9.34
CHEMBL3969707 — — 1 9.31
CHEMBL3932266 — — 1 9.28
CHEMBL3915056 — — 1 9.24
CHEMBL3936102 — — 1 9.23
CHEMBL3939751 — — 1 9.22
CHEMBL3902757 — — 1 9.15
CHEMBL3960260 — — 1 9.11
CHEMBL3929315 — — 1 9.09
CHEMBL3981662 — — 1 9.09
CHEMBL3945000 — — 1 9.08
CHEMBL3896252 — — 1 9.08
CHEMBL3921449 — — 1 9.07
CHEMBL3940191 — — 1 9.05
CHEMBL3919367 — — 1 9.05
CHEMBL3981472 — — 1 9.02
CHEMBL3981666 — — 1 9.01
CHEMBL3986775 — — 1 9.00
CHEMBL3920411 — — 1 9.00
CHEMBL3924077 — — 1 8.96
CHEMBL3914907 — — 1 8.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3892880 — IC50 = 0.168 nM 9.78
CHEMBL3917178 — IC50 = 0.3 nM 9.52
CHEMBL3929615 — IC50 = 0.3 nM 9.52
CHEMBL3953815 — IC50 = 0.3 nM 9.52
CHEMBL3946496 — IC50 = 0.32 nM 9.49
CHEMBL3915577 — IC50 = 0.32 nM 9.49
CHEMBL3944715 — IC50 = 0.391 nM 9.41
CHEMBL3986700 — IC50 = 0.4 nM 9.40
CHEMBL3936548 — IC50 = 0.4 nM 9.40
CHEMBL3938280 — IC50 = 0.456 nM 9.34
CHEMBL3969707 — IC50 = 0.4938 nM 9.31
CHEMBL3932266 — IC50 = 0.53 nM 9.28
CHEMBL3915056 — IC50 = 0.58 nM 9.24
CHEMBL3936102 — IC50 = 0.59 nM 9.23
CHEMBL3939751 — IC50 = 0.6 nM 9.22
CHEMBL3902757 — IC50 = 0.7 nM 9.15
CHEMBL3960260 — IC50 = 0.77 nM 9.11
CHEMBL3929315 — IC50 = 0.81 nM 9.09
CHEMBL3981662 — IC50 = 0.813 nM 9.09
CHEMBL3945000 — IC50 = 0.84 nM 9.08
CHEMBL3896252 — IC50 = 0.83 nM 9.08
CHEMBL3921449 — IC50 = 0.86 nM 9.07
CHEMBL3940191 — IC50 = 0.9 nM 9.05
CHEMBL3919367 — IC50 = 0.881 nM 9.05
CHEMBL3981472 — IC50 = 0.952 nM 9.02
CHEMBL3981666 — IC50 = 0.981 nM 9.01
CHEMBL3920411 — IC50 = 0.996 nM 9.00
CHEMBL3986775 — IC50 = 0.991 nM 9.00
CHEMBL3924077 — IC50 = 1.093 nM 8.96
CHEMBL3914907 — IC50 = 1.134 nM 8.95
CHEMBL3967479 — IC50 = 1.171 nM 8.93
CHEMBL3897705 — IC50 = 1.338 nM 8.87
CHEMBL3963068 — IC50 = 1.398 nM 8.85
CHEMBL3908067 — IC50 = 1.5 nM 8.82
CHEMBL1779202 — IC50 = 1.53 nM 8.81
CHEMBL4106737 — IC50 = 1.6 nM 8.80
CHEMBL3891393 — IC50 = 1.57 nM 8.80
CHEMBL3941123 — IC50 = 1.625 nM 8.79
CHEMBL3943227 — IC50 = 1.681 nM 8.77
CHEMBL3974835 — IC50 = 1.77 nM 8.75
CHEMBL3937655 — IC50 = 1.778 nM 8.75
CHEMBL3890509 — IC50 = 1.837 nM 8.74
CHEMBL3978878 — IC50 = 1.864 nM 8.73
CHEMBL3911685 — IC50 = 1.891 nM 8.72
CHEMBL3948122 — IC50 = 1.93 nM 8.71
CHEMBL3972824 — IC50 = 2.001 nM 8.70
CHEMBL3892424 — IC50 = 2.052 nM 8.69
CHEMBL3976640 — IC50 = 2.099 nM 8.68
CHEMBL3961470 — IC50 = 2.115 nM 8.68
CHEMBL3983337 — IC50 = 2.2 nM 8.66