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Assay Detail

CHEMBL1832515

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Binding
Inhibition of full length recombinant HDAC1 using Fluor de Lys as substrate by fluorescence assay
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histone deacetylase 1 (CHEMBL325) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
Wang H, Yu N, Chen D, Lee KC, Lye PL, Chang JW, Deng W, Ng MC, Lu T, Khoo ML, Poulsen A, Sangthongpitag K, Wu X, Hu C, Goh KC, Wang X, Fang L, Goh KL, Khng HH, Goh SK, Yeo P, Liu X, Bonday Z, Wood JM, Dymock BW, Kantharaj E, Sun ET.
J Med Chem (2011) 54 : 4694 -4720
PubMed 21634430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 7.15 8.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483254 PANOBINOSTAT 4.0 1 8.17
CHEMBL1830534 — — 1 7.82
CHEMBL1830420 — — 1 7.70
CHEMBL1830536 — — 1 7.68
CHEMBL1830535 — — 1 7.66
CHEMBL489332 — — 1 7.64
CHEMBL1830540 — — 1 7.64
CHEMBL1830418 — — 1 7.57
CHEMBL1830424 — — 1 7.55
CHEMBL1830533 — — 1 7.54
CHEMBL491316 — — 1 7.54
CHEMBL1830537 — — 1 7.52
CHEMBL1830541 — — 1 7.50
CHEMBL1830422 — — 1 7.44
CHEMBL1830539 — — 1 7.43
CHEMBL1830405 — — 1 7.39
CHEMBL1830419 — — 1 7.39
CHEMBL1830532 — — 1 7.39
CHEMBL1830396 — — 1 7.38
CHEMBL460963 — — 1 7.38
CHEMBL1830414 — — 1 7.35
CHEMBL1830421 — — 1 7.35
CHEMBL1830397 — — 1 7.34
CHEMBL1830538 — — 1 7.28
CHEMBL491491 — — 1 7.28
CHEMBL408513 BELINOSTAT 4.0 1 7.20
CHEMBL1830403 — — 1 7.17
CHEMBL3215861 — — 1 7.11
CHEMBL1830416 — — 1 7.11
CHEMBL1830413 — — 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483254 PANOBINOSTAT IC50 = 6.8 nM 8.17
CHEMBL1830534 — IC50 = 15.0 nM 7.82
CHEMBL1830420 — IC50 = 20.0 nM 7.70
CHEMBL1830536 — IC50 = 21.0 nM 7.68
CHEMBL1830535 — IC50 = 22.0 nM 7.66
CHEMBL489332 — IC50 = 23.0 nM 7.64
CHEMBL1830540 — IC50 = 23.0 nM 7.64
CHEMBL1830418 — IC50 = 27.0 nM 7.57
CHEMBL1830424 — IC50 = 28.0 nM 7.55
CHEMBL1830533 — IC50 = 29.0 nM 7.54
CHEMBL491316 — IC50 = 29.0 nM 7.54
CHEMBL1830537 — IC50 = 30.0 nM 7.52
CHEMBL1830541 — IC50 = 32.0 nM 7.50
CHEMBL1830422 — IC50 = 36.0 nM 7.44
CHEMBL1830539 — IC50 = 37.0 nM 7.43
CHEMBL1830405 — IC50 = 41.0 nM 7.39
CHEMBL1830532 — IC50 = 41.0 nM 7.39
CHEMBL1830419 — IC50 = 41.0 nM 7.39
CHEMBL1830396 — IC50 = 42.0 nM 7.38
CHEMBL460963 — IC50 = 42.0 nM 7.38
CHEMBL1830414 — IC50 = 45.0 nM 7.35
CHEMBL1830421 — IC50 = 45.0 nM 7.35
CHEMBL1830397 — IC50 = 46.0 nM 7.34
CHEMBL1830538 — IC50 = 53.0 nM 7.28
CHEMBL491491 — IC50 = 52.0 nM 7.28
CHEMBL408513 BELINOSTAT IC50 = 63.0 nM 7.20
CHEMBL1830403 — IC50 = 68.0 nM 7.17
CHEMBL3215861 — IC50 = 77.0 nM 7.11
CHEMBL1830416 — IC50 = 77.0 nM 7.11
CHEMBL1830413 — IC50 = 84.0 nM 7.08
CHEMBL1830399 — IC50 = 90.0 nM 7.05
CHEMBL1828648 — IC50 = 92.0 nM 7.04
CHEMBL1830406 — IC50 = 105.0 nM 6.98
CHEMBL1830417 — IC50 = 109.0 nM 6.96
CHEMBL1830402 — IC50 = 110.0 nM 6.96
CHEMBL98 VORINOSTAT IC50 = 119.0 nM 6.92
CHEMBL1830407 — IC50 = 125.0 nM 6.90
CHEMBL1830398 — IC50 = 135.0 nM 6.87
CHEMBL1830393 — IC50 = 150.0 nM 6.82
CHEMBL1830415 — IC50 = 155.0 nM 6.81
CHEMBL1830408 — IC50 = 158.0 nM 6.80
CHEMBL1830395 — IC50 = 165.0 nM 6.78
CHEMBL1830411 — IC50 = 169.0 nM 6.77
CHEMBL1830412 — IC50 = 175.0 nM 6.76
CHEMBL1830394 — IC50 = 175.0 nM 6.76
CHEMBL1830404 — IC50 = 190.0 nM 6.72
CHEMBL1830409 — IC50 = 308.0 nM 6.51
CHEMBL1830423 — IC50 = 335.0 nM 6.47
CHEMBL1830410 — IC50 = 421.0 nM 6.38
CHEMBL1830401 — IC50 = 575.0 nM 6.24