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Assay Detail

CHEMBL5738408

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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 ↗
357
Total Activities
68
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 JAK3 (CHEMBL2148) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aryl cyclopropyl-amino-isoquinolinyl amide compounds
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
kon 119 - -
k_off 119 - -
IC50 118 7.61 9.40
Ki 1 6.68 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5925417 — — 15 9.40
CHEMBL5997512 — — 6 9.40
CHEMBL5824125 — — 9 9.40
CHEMBL6063322 — — 3 9.05
CHEMBL5878871 — — 6 9.00
CHEMBL5997138 — — 18 8.82
CHEMBL5952462 — — 3 8.72
CHEMBL5746813 — — 3 8.72
CHEMBL5974947 — — 6 8.62
CHEMBL5989194 — — 12 8.54
CHEMBL5859880 — — 3 8.41
CHEMBL5787843 — — 6 8.38
CHEMBL5892273 — — 6 8.36
CHEMBL5987641 — — 6 8.33
CHEMBL5752673 — — 6 8.32
CHEMBL5910422 — — 9 8.24
CHEMBL6007723 — — 6 8.20
CHEMBL5762387 — — 6 8.09
CHEMBL5783803 — — 9 8.05
CHEMBL5994968 — — 3 7.98
CHEMBL5963304 — — 3 7.92
CHEMBL5969847 — — 3 7.89
CHEMBL5869094 — — 6 7.89
CHEMBL5899583 — — 9 7.85
CHEMBL5919378 — — 3 7.84
CHEMBL5773485 — — 3 7.82
CHEMBL5962418 — — 3 7.82
CHEMBL5811883 — — 6 7.82
CHEMBL5883781 — — 3 7.80
CHEMBL5834676 — — 6 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5925417 — IC50 = 0.4 nM 9.40
CHEMBL5824125 — IC50 = 0.4 nM 9.40
CHEMBL5997512 — IC50 = 0.4 nM 9.40
CHEMBL6063322 — IC50 = 0.9 nM 9.05
CHEMBL5878871 — IC50 = 1.0 nM 9.00
CHEMBL5997138 — IC50 = 1.5 nM 8.82
CHEMBL5997138 — IC50 = 1.5 nM 8.82
CHEMBL5997138 — IC50 = 1.5 nM 8.82
CHEMBL5997138 — IC50 = 1.5 nM 8.82
CHEMBL5952462 — IC50 = 1.9 nM 8.72
CHEMBL5746813 — IC50 = 1.9 nM 8.72
CHEMBL5878871 — IC50 = 1.9 nM 8.72
CHEMBL5974947 — IC50 = 2.4 nM 8.62
CHEMBL5824125 — IC50 = 2.4 nM 8.62
CHEMBL5989194 — IC50 = 2.9 nM 8.54
CHEMBL5997138 — IC50 = 2.9 nM 8.54
CHEMBL5997138 — IC50 = 2.9 nM 8.54
CHEMBL5974947 — IC50 = 2.9 nM 8.54
CHEMBL5925417 — IC50 = 2.9 nM 8.54
CHEMBL5824125 — IC50 = 3.4 nM 8.47
CHEMBL5859880 — IC50 = 3.9 nM 8.41
CHEMBL5787843 — IC50 = 4.2 nM 8.38
CHEMBL5787843 — IC50 = 4.3 nM 8.37
CHEMBL5892273 — IC50 = 4.4 nM 8.36
CHEMBL5987641 — IC50 = 4.7 nM 8.33
CHEMBL5989194 — IC50 = 4.8 nM 8.32
CHEMBL5989194 — IC50 = 4.8 nM 8.32
CHEMBL5752673 — IC50 = 4.8 nM 8.32
CHEMBL5752673 — IC50 = 4.8 nM 8.32
CHEMBL5989194 — IC50 = 4.8 nM 8.32
CHEMBL5910422 — IC50 = 5.8 nM 8.24
CHEMBL5910422 — IC50 = 5.8 nM 8.24
CHEMBL5910422 — IC50 = 5.8 nM 8.24
CHEMBL6007723 — IC50 = 6.3 nM 8.20
CHEMBL6007723 — IC50 = 6.3 nM 8.20
CHEMBL5892273 — IC50 = 6.8 nM 8.17
CHEMBL5925417 — IC50 = 7.4 nM 8.13
CHEMBL5925417 — IC50 = 7.4 nM 8.13
CHEMBL5925417 — IC50 = 7.4 nM 8.13
CHEMBL5997512 — IC50 = 7.7 nM 8.11
CHEMBL5762387 — IC50 = 8.2 nM 8.09
CHEMBL5762387 — IC50 = 8.2 nM 8.09
CHEMBL5783803 — IC50 = 9.0 nM 8.05
CHEMBL5783803 — IC50 = 9.0 nM 8.05
CHEMBL5783803 — IC50 = 9.0 nM 8.05
CHEMBL5987641 — IC50 = 10.0 nM 8.00
CHEMBL5994968 — IC50 = 10.5 nM 7.98
CHEMBL5963304 — IC50 = 12.0 nM 7.92
CHEMBL5969847 — IC50 = 13.0 nM 7.89
CHEMBL5869094 — IC50 = 13.0 nM 7.89