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Assay Detail

CHEMBL5736216

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Binding
LanthaScreen Eu Kinase Binding Assay: Table 3: Small molecules were tested for their inhibitory activities towards casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ϵ). The in vitro LanthaScreen Eu kinase binding assay was used to determine the IC50 values for 15 of the synthesized compounds and 5 commercial inhibitors including SB203580 (Table 3). Tested compounds displayed a wide range of affinity between 6.8 nM (high affinity=strong inhibition) to values over 1000 nM (low affinity=very weak inhibition).
ChEMBL ↗
60
Total Activities
20
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Casein kinase I isoform epsilon (CHEMBL4937) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.69 8.19
kon 20 - -
k_off 20 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4303658 — — 3 8.19
CHEMBL5303421 — — 3 7.80
CHEMBL5941528 — — 3 7.50
CHEMBL2385554 — — 3 7.36
CHEMBL10 SB-203580 — 3 7.20
CHEMBL278041 SB-202190 — 3 7.08
CHEMBL410456 — — 3 7.06
CHEMBL363648 TAK-715 2.0 3 6.97
CHEMBL440084 SB-431542 — 3 6.83
CHEMBL2385555 — — 3 6.82
CHEMBL2385551 — — 3 6.56
CHEMBL2385557 — — 3 6.56
CHEMBL5963663 — — 3 6.53
CHEMBL6031723 — — 3 6.52
CHEMBL2385556 — — 3 6.39
CHEMBL5891266 — — 3 6.12
CHEMBL6006706 — — 3 5.97
CHEMBL6054487 — — 3 5.94
CHEMBL2385553 — — 3 5.25
CHEMBL2385552 — — 3 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4303658 — IC50 = 6.4 nM 8.19
CHEMBL5303421 — IC50 = 16.0 nM 7.80
CHEMBL5941528 — IC50 = 32.0 nM 7.50
CHEMBL2385554 — IC50 = 44.0 nM 7.36
CHEMBL10 SB-203580 IC50 = 63.0 nM 7.20
CHEMBL278041 SB-202190 IC50 = 83.0 nM 7.08
CHEMBL410456 — IC50 = 88.0 nM 7.06
CHEMBL363648 TAK-715 IC50 = 107.0 nM 6.97
CHEMBL440084 SB-431542 IC50 = 147.0 nM 6.83
CHEMBL2385555 — IC50 = 150.0 nM 6.82
CHEMBL2385557 — IC50 = 277.0 nM 6.56
CHEMBL2385551 — IC50 = 274.0 nM 6.56
CHEMBL5963663 — IC50 = 295.0 nM 6.53
CHEMBL6031723 — IC50 = 300.0 nM 6.52
CHEMBL2385556 — IC50 = 411.0 nM 6.39
CHEMBL5891266 — IC50 = 751.0 nM 6.12
CHEMBL6006706 — IC50 = 1061.0 nM 5.97
CHEMBL6054487 — IC50 = 1145.0 nM 5.94
CHEMBL2385553 — IC50 = 5610.0 nM 5.25
CHEMBL2385552 — IC50 = 5891.0 nM 5.23
CHEMBL410456 — kon = - — -
CHEMBL6054487 — k_off = - s-1 -
CHEMBL10 SB-203580 kon = - — -
CHEMBL10 SB-203580 k_off = - s-1 -
CHEMBL278041 SB-202190 kon = - — -
CHEMBL278041 SB-202190 k_off = - s-1 -
CHEMBL2385557 — kon = - — -
CHEMBL2385557 — k_off = - s-1 -
CHEMBL2385553 — kon = - — -
CHEMBL2385553 — k_off = - s-1 -
CHEMBL2385555 — kon = - — -
CHEMBL2385555 — k_off = - s-1 -
CHEMBL6054487 — kon = - — -
CHEMBL5303421 — k_off = - s-1 -
CHEMBL5891266 — kon = - — -
CHEMBL363648 TAK-715 k_off = - s-1 -
CHEMBL363648 TAK-715 kon = - — -
CHEMBL6031723 — k_off = - s-1 -
CHEMBL6031723 — kon = - — -
CHEMBL6006706 — k_off = - s-1 -
CHEMBL6006706 — kon = - — -
CHEMBL5963663 — k_off = - s-1 -
CHEMBL5963663 — kon = - — -
CHEMBL440084 SB-431542 k_off = - s-1 -
CHEMBL4303658 — k_off = - s-1 -
CHEMBL4303658 — kon = - — -
CHEMBL410456 — k_off = - s-1 -
CHEMBL5941528 — k_off = - s-1 -
CHEMBL5941528 — kon = - — -
CHEMBL440084 SB-431542 kon = - — -