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Assay Detail

CHEMBL3707950

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Binding
In Vitro Enzyme Assay: The ability of compounds to inhibit the kinase activity of baculovirus-expressed human FAK and JAK kinase using the time-resolved fluorescence (TRF) assay system.
ChEMBL ↗
363
Total Activities
361
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 363 7.32 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3642343 — — 1 9.57
CHEMBL2062802 — — 1 9.40
CHEMBL3642405 — — 1 9.39
CHEMBL3642411 — — 1 9.34
CHEMBL3644960 — — 1 9.30
CHEMBL3642344 — — 1 9.26
CHEMBL3642412 — — 1 9.26
CHEMBL3642296 — — 1 9.22
CHEMBL3642262 — — 1 9.22
CHEMBL3642295 — — 1 9.22
CHEMBL3639411 — — 1 9.22
CHEMBL3642404 — — 1 9.19
CHEMBL3642340 — — 1 9.18
CHEMBL2062807 — — 1 9.17
CHEMBL3642258 — — 1 9.15
CHEMBL3644961 — — 1 9.15
CHEMBL3642285 — — 1 9.15
CHEMBL2062809 — — 1 9.15
CHEMBL3642389 — — 1 9.14
CHEMBL3642365 — — 1 9.12
CHEMBL3642339 — — 1 9.12
CHEMBL3642303 — — 1 9.10
CHEMBL2062803 — — 1 9.05
CHEMBL3642341 — — 1 9.02
CHEMBL3642402 — — 1 9.01
CHEMBL3642256 — — 1 9.00
CHEMBL3642324 — — 1 9.00
CHEMBL2062799 — — 1 9.00
CHEMBL2062798 — — 1 9.00
CHEMBL3642274 — — 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3642343 — IC50 = 0.27 nM 9.57
CHEMBL2062802 — IC50 = 0.4 nM 9.40
CHEMBL3642405 — IC50 = 0.41 nM 9.39
CHEMBL3642411 — IC50 = 0.46 nM 9.34
CHEMBL3644960 — IC50 = 0.5 nM 9.30
CHEMBL3642344 — IC50 = 0.55 nM 9.26
CHEMBL3642412 — IC50 = 0.55 nM 9.26
CHEMBL3642296 — IC50 = 0.6 nM 9.22
CHEMBL3642262 — IC50 = 0.6 nM 9.22
CHEMBL3639411 — IC50 = 0.6 nM 9.22
CHEMBL3642295 — IC50 = 0.6 nM 9.22
CHEMBL3642404 — IC50 = 0.65 nM 9.19
CHEMBL3642340 — IC50 = 0.66 nM 9.18
CHEMBL2062807 — IC50 = 0.67 nM 9.17
CHEMBL3642258 — IC50 = 0.7 nM 9.15
CHEMBL3644961 — IC50 = 0.71 nM 9.15
CHEMBL2062809 — IC50 = 0.7 nM 9.15
CHEMBL3642285 — IC50 = 0.7 nM 9.15
CHEMBL3642389 — IC50 = 0.73 nM 9.14
CHEMBL3642339 — IC50 = 0.75 nM 9.12
CHEMBL3642365 — IC50 = 0.75 nM 9.12
CHEMBL3642303 — IC50 = 0.8 nM 9.10
CHEMBL2062803 — IC50 = 0.9 nM 9.05
CHEMBL3642341 — IC50 = 0.95 nM 9.02
CHEMBL3642402 — IC50 = 0.97 nM 9.01
CHEMBL2062799 — IC50 = 1.0 nM 9.00
CHEMBL3642256 — IC50 = 1.0 nM 9.00
CHEMBL3642274 — IC50 = 1.0 nM 9.00
CHEMBL3642324 — IC50 = 1.0 nM 9.00
CHEMBL2062798 — IC50 = 1.0 nM 9.00
CHEMBL3645015 — IC50 = 1.06 nM 8.97
CHEMBL3642287 — IC50 = 1.1 nM 8.96
CHEMBL3642314 — IC50 = 1.1 nM 8.96
CHEMBL3642302 — IC50 = 1.1 nM 8.96
CHEMBL3642366 — IC50 = 1.13 nM 8.95
CHEMBL3642268 — IC50 = 1.3 nM 8.89
CHEMBL3642306 — IC50 = 1.3 nM 8.89
CHEMBL2062804 — IC50 = 1.3 nM 8.89
CHEMBL2062801 — IC50 = 1.3 nM 8.89
CHEMBL2062810 — IC50 = 1.3 nM 8.89
CHEMBL3642407 — IC50 = 1.35 nM 8.87
CHEMBL3642322 — IC50 = 1.4 nM 8.85
CHEMBL3642342 — IC50 = 1.43 nM 8.85
CHEMBL3642409 — IC50 = 1.43 nM 8.85
CHEMBL2062529 — IC50 = 1.5 nM 8.82
CHEMBL3642368 — IC50 = 1.55 nM 8.81
CHEMBL3642424 — IC50 = 1.63 nM 8.79
CHEMBL3645118 — IC50 = 1.62 nM 8.79
CHEMBL3642315 — IC50 = 1.7 nM 8.77
CHEMBL3642290 — IC50 = 1.7 nM 8.77