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Assay Detail

CHEMBL5541887

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Binding
Inhibition of human recombinant CITK kinase domain assessed as phosphorylation of substrate ULight-ARTKQTARKSTGGKAPRICQLAGC measured after 30 mins by LANCE TR-FRET assay
ChEMBL ↗
61
Total Activities
61
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

Citron Rho-interacting kinase (CHEMBL5579) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of Selective, First-in-Class Inhibitors of Citron Kinase.
Maw JJ, Coker JA, Arya T, Goins CM, Sonawane D, Han SH, Rees MG, Ronan MM, Roth JA, Wang NS, Heemers HV, Macdonald JD, Stauffer SR.
J Med Chem (2024) 67 : 2631 -2666
PubMed 38330278 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 7.04 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5591534 — — 1 8.26
CHEMBL5568742 — — 1 8.00
CHEMBL5572737 — — 1 7.92
CHEMBL5595104 — — 1 7.89
CHEMBL5575901 — — 1 7.85
CHEMBL5569359 — — 1 7.82
CHEMBL5575300 — — 1 7.80
CHEMBL5579704 — — 1 7.80
CHEMBL5595678 — — 1 7.77
CHEMBL5590268 — — 1 7.77
CHEMBL5575657 — — 1 7.75
CHEMBL5574799 — — 1 7.70
CHEMBL5566667 — — 1 7.68
CHEMBL5562828 — — 1 7.51
CHEMBL5566783 — — 1 7.51
CHEMBL5542511 — — 1 7.43
CHEMBL5574511 — — 1 7.43
CHEMBL5573191 — — 1 7.41
CHEMBL5563128 — — 1 7.40
CHEMBL5574143 — — 1 7.40
CHEMBL5571250 — — 1 7.40
CHEMBL5571047 — — 1 7.40
CHEMBL5572919 — — 1 7.38
CHEMBL5563995 — — 1 7.32
CHEMBL5574850 — — 1 7.27
CHEMBL5570381 — — 1 7.21
CHEMBL5590500 — — 1 7.18
CHEMBL5574584 — — 1 7.17
CHEMBL5566515 — — 1 7.10
CHEMBL5571741 — — 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5591534 — IC50 = 5.5 nM 8.26
CHEMBL5568742 — IC50 = 10.0 nM 8.00
CHEMBL5572737 — IC50 = 12.0 nM 7.92
CHEMBL5595104 — IC50 = 13.0 nM 7.89
CHEMBL5575901 — IC50 = 14.0 nM 7.85
CHEMBL5569359 — IC50 = 15.0 nM 7.82
CHEMBL5575300 — IC50 = 16.0 nM 7.80
CHEMBL5579704 — IC50 = 16.0 nM 7.80
CHEMBL5595678 — IC50 = 17.0 nM 7.77
CHEMBL5590268 — IC50 = 17.0 nM 7.77
CHEMBL5575657 — IC50 = 18.0 nM 7.75
CHEMBL5574799 — IC50 = 20.0 nM 7.70
CHEMBL5566667 — IC50 = 21.0 nM 7.68
CHEMBL5566783 — IC50 = 31.0 nM 7.51
CHEMBL5562828 — IC50 = 31.0 nM 7.51
CHEMBL5542511 — IC50 = 37.0 nM 7.43
CHEMBL5574511 — IC50 = 37.0 nM 7.43
CHEMBL5573191 — IC50 = 39.0 nM 7.41
CHEMBL5563128 — IC50 = 40.0 nM 7.40
CHEMBL5574143 — IC50 = 40.0 nM 7.40
CHEMBL5571250 — IC50 = 40.0 nM 7.40
CHEMBL5571047 — IC50 = 40.0 nM 7.40
CHEMBL5572919 — IC50 = 42.0 nM 7.38
CHEMBL5563995 — IC50 = 48.0 nM 7.32
CHEMBL5574850 — IC50 = 54.0 nM 7.27
CHEMBL5570381 — IC50 = 61.0 nM 7.21
CHEMBL5590500 — IC50 = 66.0 nM 7.18
CHEMBL5574584 — IC50 = 67.0 nM 7.17
CHEMBL5566515 — IC50 = 80.0 nM 7.10
CHEMBL5571741 — IC50 = 90.0 nM 7.05
CHEMBL5566014 — IC50 = 89.0 nM 7.05
CHEMBL5572680 — IC50 = 92.0 nM 7.04
CHEMBL5575031 — IC50 = 110.0 nM 6.96
CHEMBL5590585 — IC50 = 110.0 nM 6.96
CHEMBL5583840 — IC50 = 130.0 nM 6.89
CHEMBL571948 Y-39983 IC50 = 150.0 nM 6.82
CHEMBL5564045 — IC50 = 160.0 nM 6.80
CHEMBL5575191 — IC50 = 160.0 nM 6.80
CHEMBL5566310 — IC50 = 170.0 nM 6.77
CHEMBL5569087 — IC50 = 210.0 nM 6.68
CHEMBL5574968 — IC50 = 250.0 nM 6.60
CHEMBL5571124 — IC50 = 280.0 nM 6.55
CHEMBL5595129 — IC50 = 320.0 nM 6.50
CHEMBL5574306 — IC50 = 330.0 nM 6.48
CHEMBL5565388 — IC50 = 340.0 nM 6.47
CHEMBL5574767 — IC50 = 410.0 nM 6.39
CHEMBL5571901 — IC50 = 500.0 nM 6.30
CHEMBL5573912 — IC50 = 520.0 nM 6.28
CHEMBL5574220 — IC50 = 620.0 nM 6.21
CHEMBL5590106 — IC50 = 700.0 nM 6.16