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Assay Detail

CHEMBL5738407

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Binding
JAK Kinase Assays: Compounds were prepared in the exact same manner as described in the ROCK Kinase Assay with the exception to the substrate and enzyme. The JAK 2× substrate/enzyme solution consisted of acceptor substrate (800 nM Abl peptide EAIYAAPFAKKK (SEQ ID NO: 2)), JAK2 or JAK3 enzyme (10 nM) and DTT (2 μM). All other steps and solutions remain identical to the ROCK Kinase Assay above.
ChEMBL ↗
363
Total Activities
70
Compounds Tested
4
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

Aryl cyclopropyl-amino-isoquinolinyl amide compounds
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
kon 121 - -
k_off 121 - -
IC50 120 8.30 9.46
Ki 1 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5824125 — — 9 9.46
CHEMBL5834676 — — 6 9.40
CHEMBL5987641 — — 6 9.22
CHEMBL6063322 — — 3 9.19
CHEMBL5859880 — — 3 9.19
CHEMBL5878871 — — 6 9.15
CHEMBL5997138 — — 18 9.15
CHEMBL5787843 — — 6 9.10
CHEMBL5974947 — — 6 9.05
CHEMBL5811883 — — 6 9.05
CHEMBL5783803 — — 9 9.05
CHEMBL5997512 — — 6 9.02
CHEMBL5952462 — — 3 9.02
CHEMBL5989194 — — 12 9.00
CHEMBL5892273 — — 6 9.00
CHEMBL5919378 — — 3 9.00
CHEMBL5752673 — — 6 9.00
CHEMBL5910422 — — 9 9.00
CHEMBL5869094 — — 6 9.00
CHEMBL5762387 — — 6 9.00
CHEMBL5925417 — — 15 9.00
CHEMBL5954872 — — 9 8.94
CHEMBL5856025 — — 6 8.85
CHEMBL5883781 — — 3 8.70
CHEMBL5746813 — — 3 8.70
CHEMBL5994968 — — 3 8.70
CHEMBL5963304 — — 3 8.70
CHEMBL5957627 — — 6 8.70
CHEMBL6007723 — — 6 8.70
CHEMBL5935057 — — 6 8.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5824125 — IC50 = 0.35 nM 9.46
CHEMBL5824125 — IC50 = 0.35 nM 9.46
CHEMBL5824125 — IC50 = 0.35 nM 9.46
CHEMBL5834676 — IC50 = 0.4 nM 9.40
CHEMBL5834676 — IC50 = 0.4 nM 9.40
CHEMBL5987641 — IC50 = 0.6 nM 9.22
CHEMBL6063322 — IC50 = 0.65 nM 9.19
CHEMBL5859880 — IC50 = 0.65 nM 9.19
CHEMBL5878871 — IC50 = 0.7 nM 9.15
CHEMBL5997138 — IC50 = 0.7 nM 9.15
CHEMBL5997138 — IC50 = 0.7 nM 9.15
CHEMBL5997138 — IC50 = 0.7 nM 9.15
CHEMBL5997138 — IC50 = 0.7 nM 9.15
CHEMBL5787843 — IC50 = 0.8 nM 9.10
CHEMBL5787843 — IC50 = 0.8 nM 9.10
CHEMBL5974947 — IC50 = 0.9 nM 9.05
CHEMBL5974947 — IC50 = 0.9 nM 9.05
CHEMBL5811883 — IC50 = 0.9 nM 9.05
CHEMBL5783803 — IC50 = 0.9 nM 9.05
CHEMBL5783803 — IC50 = 0.9 nM 9.05
CHEMBL5783803 — IC50 = 0.9 nM 9.05
CHEMBL5997512 — IC50 = 0.95 nM 9.02
CHEMBL5952462 — IC50 = 0.95 nM 9.02
CHEMBL5762387 — IC50 = 1.0 nM 9.00
CHEMBL5762387 — IC50 = 1.0 nM 9.00
CHEMBL5869094 — IC50 = 1.0 nM 9.00
CHEMBL5878871 — IC50 = 1.0 nM 9.00
CHEMBL5910422 — IC50 = 1.0 nM 9.00
CHEMBL5752673 — IC50 = 1.0 nM 9.00
CHEMBL5910422 — IC50 = 1.0 nM 9.00
CHEMBL5910422 — IC50 = 1.0 nM 9.00
CHEMBL5919378 — IC50 = 1.0 nM 9.00
CHEMBL5989194 — IC50 = 1.0 nM 9.00
CHEMBL5925417 — IC50 = 1.0 nM 9.00
CHEMBL5752673 — IC50 = 1.0 nM 9.00
CHEMBL5892273 — IC50 = 1.0 nM 9.00
CHEMBL5925417 — IC50 = 1.0 nM 9.00
CHEMBL5954872 — IC50 = 1.15 nM 8.94
CHEMBL5954872 — IC50 = 1.15 nM 8.94
CHEMBL5954872 — IC50 = 1.2 nM 8.92
CHEMBL5856025 — IC50 = 1.4 nM 8.85
CHEMBL5892273 — IC50 = 1.5 nM 8.82
CHEMBL5997138 — IC50 = 1.5 nM 8.82
CHEMBL5856025 — IC50 = 1.5 nM 8.82
CHEMBL5811883 — IC50 = 1.5 nM 8.82
CHEMBL5997138 — IC50 = 1.5 nM 8.82
CHEMBL5987641 — IC50 = 2.0 nM 8.70
CHEMBL5957627 — IC50 = 2.0 nM 8.70
CHEMBL5963304 — IC50 = 2.0 nM 8.70
CHEMBL5989194 — IC50 = 2.0 nM 8.70