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Assay Detail

CHEMBL4386404

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of tubastatin-Alexa647-tracer binding to recombinant GST-tagged HDAC10 (unknown origin) measured after 1 hr by TR-FRET assay
29
Total Activities
29
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

Polyamine deacetylase HDAC10 (CHEMBL5103)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated.
Géraldy M, Morgen M, Sehr P, Steimbach RR, Moi D, Ridinger J, Oehme I, Witt O, Malz M, Nogueira MS, Koch O, Gunkel N, Miller AK.
J Med Chem (2019) 62 : 4426 -4443
PubMed 30964290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.92 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4578278 1 8.40
CHEMBL2103863 ABEXINOSTAT 3.0 1 8.40
CHEMBL4532181 1 8.30
CHEMBL4066920 1 8.30
CHEMBL2105763 QUISINOSTAT 2.0 1 8.00
CHEMBL2018302 TUBASTATIN A 1 7.90
CHEMBL3907295 1 7.70
CHEMBL4470067 1 7.70
CHEMBL4541796 1 7.60
CHEMBL3958794 1 7.20
CHEMBL4466930 1 7.10
CHEMBL4066043 1 7.10
CHEMBL2179618 NEXTURASTAT A 1 7.00
CHEMBL4445881 1 6.90
CHEMBL598797 CUDC-101 1.0 1 6.90
CHEMBL2364628 RICOLINOSTAT 2.0 1 6.90
CHEMBL4534503 1 6.80
CHEMBL2018451 1 6.70
CHEMBL98 VORINOSTAT 4.0 1 6.70
CHEMBL3971436 1 6.50
CHEMBL4438279 1 6.50
CHEMBL511749 1 6.50
CHEMBL4562244 1 6.30
CHEMBL4531802 1 6.20
CHEMBL4475240 1 6.00
CHEMBL1851943 PRACINOSTAT 3.0 1 5.80
CHEMBL2170166 1 5.70
CHEMBL4468860 1 5.30
CHEMBL2170177 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4578278 IC50 = 3.981 nM 8.40
CHEMBL2103863 ABEXINOSTAT IC50 = 3.981 nM 8.40
CHEMBL4532181 IC50 = 5.012 nM 8.30
CHEMBL4066920 IC50 = 5.012 nM 8.30
CHEMBL2105763 QUISINOSTAT IC50 = 10.0 nM 8.00
CHEMBL2018302 TUBASTATIN A IC50 = 12.59 nM 7.90
CHEMBL3907295 IC50 = 19.95 nM 7.70
CHEMBL4470067 IC50 = 19.95 nM 7.70
CHEMBL4541796 IC50 = 25.12 nM 7.60
CHEMBL3958794 IC50 = 63.1 nM 7.20
CHEMBL4466930 IC50 = 79.43 nM 7.10
CHEMBL4066043 IC50 = 79.43 nM 7.10
CHEMBL2179618 NEXTURASTAT A IC50 = 100.0 nM 7.00
CHEMBL4445881 IC50 = 125.89 nM 6.90
CHEMBL598797 CUDC-101 IC50 = 125.89 nM 6.90
CHEMBL2364628 RICOLINOSTAT IC50 = 125.89 nM 6.90
CHEMBL4534503 IC50 = 158.49 nM 6.80
CHEMBL2018451 IC50 = 199.53 nM 6.70
CHEMBL98 VORINOSTAT IC50 = 199.53 nM 6.70
CHEMBL3971436 IC50 = 316.23 nM 6.50
CHEMBL4438279 IC50 = 316.23 nM 6.50
CHEMBL511749 IC50 = 316.23 nM 6.50
CHEMBL4562244 IC50 = 501.19 nM 6.30
CHEMBL4531802 IC50 = 630.96 nM 6.20
CHEMBL4475240 IC50 = 1000.0 nM 6.00
CHEMBL1851943 PRACINOSTAT IC50 = 1584.89 nM 5.80
CHEMBL2170166 IC50 = 1995.26 nM 5.70
CHEMBL4468860 IC50 = 5011.87 nM 5.30
CHEMBL2170177 IC50 = 39810.72 nM 4.40