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Assay Detail

CHEMBL5738809

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Binding
Enzymatic Assay: The IC50 values for aforementioned compounds against HDACs were determined. HDAC 1 to 11 can be assayed by using acetylated AMC-labeled peptide substrate. The Substrate 1, a fluorogenic peptide from p53 residues 379-382 (RHKKAc) is used for all MAC 1 to 11 but HDAC8, which has a substrate II (RHKAcKAc), a fluorogenic diacyl peptide based on residues 179-382 of p53. Compounds were tested in 10-dose 1050 mode in duplicate with 3-fold serial dilution starting at 10 uM.
ChEMBL ↗
78
Total Activities
25
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 8 (CHEMBL3192) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Histone deacetylases (HDACs) inhibitors
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.18 7.02
kon 26 - -
k_off 26 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4579683 — — 3 7.02
CHEMBL4457790 — — 3 6.77
CHEMBL99 TRICHOSTATIN 1.0 6 6.76
CHEMBL5914638 — — 3 6.63
CHEMBL5759520 — — 3 6.54
CHEMBL4550214 — — 3 6.42
CHEMBL5396951 — — 3 6.40
CHEMBL4442777 — — 3 6.37
CHEMBL5968609 — — 3 6.31
CHEMBL5822037 — — 3 6.28
CHEMBL4554270 — — 3 6.28
CHEMBL4473726 — — 3 6.18
CHEMBL4537684 — — 3 6.14
CHEMBL5770781 — — 3 6.01
CHEMBL4453971 — — 3 5.98
CHEMBL4438057 — — 3 5.97
CHEMBL4470654 — — 3 5.94
CHEMBL4457073 — — 3 5.92
CHEMBL5436391 — — 3 5.89
CHEMBL5891478 — — 3 5.85
CHEMBL4513424 — — 3 5.84
CHEMBL4565933 — — 3 5.79
CHEMBL4517827 — — 3 5.60
CHEMBL4441436 — — 3 5.56
CHEMBL4474286 — — 3 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4579683 — IC50 = 95.0 nM 7.02
CHEMBL4457790 — IC50 = 169.0 nM 6.77
CHEMBL99 TRICHOSTATIN IC50 = 175.0 nM 6.76
CHEMBL99 TRICHOSTATIN IC50 = 175.0 nM 6.76
CHEMBL5914638 — IC50 = 235.0 nM 6.63
CHEMBL5759520 — IC50 = 287.0 nM 6.54
CHEMBL4550214 — IC50 = 376.0 nM 6.42
CHEMBL5396951 — IC50 = 400.0 nM 6.40
CHEMBL4442777 — IC50 = 428.0 nM 6.37
CHEMBL5968609 — IC50 = 486.0 nM 6.31
CHEMBL4554270 — IC50 = 525.0 nM 6.28
CHEMBL5822037 — IC50 = 523.0 nM 6.28
CHEMBL4473726 — IC50 = 653.0 nM 6.18
CHEMBL4537684 — IC50 = 731.0 nM 6.14
CHEMBL5770781 — IC50 = 979.0 nM 6.01
CHEMBL4453971 — IC50 = 1049.0 nM 5.98
CHEMBL4438057 — IC50 = 1068.0 nM 5.97
CHEMBL4470654 — IC50 = 1155.0 nM 5.94
CHEMBL4457073 — IC50 = 1191.0 nM 5.92
CHEMBL5436391 — IC50 = 1300.0 nM 5.89
CHEMBL5891478 — IC50 = 1420.0 nM 5.85
CHEMBL4513424 — IC50 = 1442.0 nM 5.84
CHEMBL4565933 — IC50 = 1640.0 nM 5.79
CHEMBL4517827 — IC50 = 2521.0 nM 5.60
CHEMBL4441436 — IC50 = 2751.0 nM 5.56
CHEMBL4474286 — IC50 = 3060.0 nM 5.51
CHEMBL4442777 — kon = - — -
CHEMBL4579683 — k_off = - s-1 -
CHEMBL4579683 — kon = - — -
CHEMBL4565933 — k_off = - s-1 -
CHEMBL99 TRICHOSTATIN kon = - — -
CHEMBL5770781 — k_off = - s-1 -
CHEMBL5770781 — kon = - — -
CHEMBL5891478 — k_off = - s-1 -
CHEMBL5891478 — kon = - — -
CHEMBL4474286 — k_off = - s-1 -
CHEMBL4474286 — kon = - — -
CHEMBL4442777 — k_off = - s-1 -
CHEMBL4457790 — k_off = - s-1 -
CHEMBL4457073 — k_off = - s-1 -
CHEMBL4457073 — kon = - — -
CHEMBL5759520 — k_off = - s-1 -
CHEMBL5759520 — kon = - — -
CHEMBL4517827 — k_off = - s-1 -
CHEMBL99 TRICHOSTATIN k_off = - s-1 -
CHEMBL5396951 — kon = - — -
CHEMBL4517827 — kon = - — -
CHEMBL5396951 — k_off = - s-1 -
CHEMBL4470654 — k_off = - s-1 -
CHEMBL4457790 — kon = - — -