South China Drug Screening Center

Intruduction
The Sourth China Drug Screening Center (SCDSC) is a drug discovery service core belonging to Guangzhou Institutes of Biomedicine and Health,Chinese Academy of Sciences, located in Science Park, Guangzhou, China. SCDSC has the art-of-the state instruments such Echeo 550, Envision microplate reader. The scientists have extensive expertise in assay development, validation and miniaturization in drug discovery.

Services
We have extensive experience to develop biochemical assays and cell based assay for customers. We offer high quality assay development and library screening, high throughput and high content screening, and complete data analysis services to investigate the major drugable target classes including kinases, proteases, HDACs, nuclear receptors， anti-influenzae, anti-EV71 virus to meet your drug discovery needs

We offer the following services:

Assay development Primary library HTS Screen Hit confirmation & characterization Library Screening Cell toxicity & viability assay Cell apoptosis assay Biochemical P450 assay Research project collaboration Drug Co-Development Drugable targets, we have experience running these assays: Protein kinases:

ABL1
ABL1(E255K)
ABL1(G250E)
ABL1(H396P)
ABL1(M351T)
ABL1(Q252H)
ABL1(T315I)
ABL1(Y253F)
ALK
AKT-1
AKT-2
AKT-3
EGFR
EGFR(L858R)
EGFR(L861Q)
EGFR(L858R,T790M)
EGFR (T790M)
Her2
Kit

Proteases
HCVNS3/4
MMP-1
ADAM10
TACE/ADAM17
DDP4
DDP8
DDP9

Other targets
COX-1
COX-2

Human HDACs
HDAC1
HDAC2
HDAC4
HDAC7

Biochemical CYP450 assay
CYP1A2
CYP2C9
CYP2C19
CYP2D6
CYP3A4

Anti-influezae
Anti-influezae inhibitor cell-based assay
NAS, NAR

ABL1
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1

• Enzyme: Human ABL1

• Assay methods: FRET， substrate, ATP 10 μM

• Inhibitor IC50 (nM)
  AG1478， 659.2
  Gleevec，272.9
  AP24534， 252.4
  Staurosporine， 156.1

• Scientific Information: P00519 (http://www.expasy.org/uniprot/P00519) 




ABL1(E255K)
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1(E255K)

• Enzyme: Human ABL1(E255K)

• Assay methods: FRET; ATP 5 μM

• Inhibitor IC50 (nM)
  Staurosporine， 165.0

• Scientific Information: P00519 (http://www.expasy.org/uniprot/P00519) 



ABL1(G250E)
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1(G250E)

• Enzyme: Human ABL1(G250E)

• Assay methods: FRET; ATP 5 μM

• Inhibitor IC50 (nM)
  Staurosporine， 70.0

• Scientific Information: P00519 (http://www.expasy.org/uniprot/P00519) 




ABL1(H396P)
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1(H396P)

• Enzyme: Human ABL1(H396P)

• Assay methods: FRET; ATP 10 μM

• Inhibitor IC50 (nM)
  Staurosporine， 110.8

• Scientific Information: P00519 (http://www.expasy.org/uniprot/P00519) 




ABL1(M351T)
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1(M351T)

• Enzyme: Human ABL1(M351T)

• Assay methods: FRET; ATP 10 μM

• Inhibitor IC50 (nM)
  Staurosporine， 52.2

• Scientific Information: P00519 (http://www.expasy.org/uniprot/P00519) 




ABL1(Q252H)
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1(Q252H)

• Enzyme: Human ABL1(Q252H)

• Assay methods: FRET; ATP 10 μM

• Inhibitor IC50 (nM)
  Staurosporine，654.5

• Scientific Information: P00519 (http://www.expasy.org/uniprot/P00519) 




ABL1 (T315I)
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1 (T315I)

• Enzyme:Human ABL1 (T315I)

• Assay methods: FRET; ATP 5 μM

• Inhibitor IC50 (nM)
  Staurosporine 24.2
  AP24534， 5.41
  Lapatinib， 155.3

• Scientific Information: P00519 (http://www.expasy.org/uniprot/P00519) 




ABL1(Y253F)
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1(Y253F)

• Enzyme: Human ABL1(Y253F)

• Assay methods: FRET; ATP 10 μM

• Inhibitor IC50 (nM)
  Staurosporine，69.6

• Scientific Information: P00519 (http://www.expasy.org/uniprot/P00519) 




AKT1
(RAC-alpha serine/threonine-protein kinase, RAC-PK-alpha, Protein kinase Bα, C-AKT) 

• CAT#: AKT1

• Enzyme: Human AKT1

• Assay methods: FRET; ATP 75 μM

• Inhibitor IC50 (nM):
  Staurosporine 102.2
  DCPOS 72.48

• Scientific Information: P31749 (http://www.expasy.org/uniprot/P31749) 




AKT2
(RAC-beta serine/threonine-protein kinase, RAC-PK-beta, Protein kinase Akt-2, Protein kinase B beta, PKBβ)

• CAT#: AKT2

• Enzyme: Human AKT2

• Assay methods: FRET; ATP 200 μM

• Inhibitor IC50 (nM):
  Staurosporine 449.5
  DCPOS 497

• Scientific Information: P31751 (http://www.expasy.org/uniprot/P31751) 




AKT3
(RAC-gamma serine/threonine-protein kinase, RAC-PK-gamma, Protein kinase Akt-3, Protein kinase B gamma, PKB gamma, STK-2)

• CAT#: AKT3

• Enzyme: Human AKT3

• Assay methods: FRET; ATP 100 μM

• Inhibitor IC50 (nM):
  Staurosporine 163
  DCPOS 63.01

• Scientific Information: Q9Y243 (http://www.expasy.org/uniprot/Q9Y243) 




ALK
(ALK tyrosine kinase receptor [Precursor], Anaplastic lymphoma kinase)

• CAT#: ALK

• Enzyme: Human ALK

• Assay methods: FRET; ATP 10 μM

• Inhibitor IC50 (nM)
  Staurosporine 19.87

• Scientific Information: Q9UM73 (http://www.expasy.org/uniprot/Q9UM73) 




Kit
(Mast/stem cell growth factor receptor, Proto-oncogene tyrosine-protein kinase c-kit)

• CAT#: Kit

• Enzyme: Human Kit

• Assay methods: FRET; ATP 300 μM

• Inhibitor IC50 (nM):
  Staurosporine 464.1

• Scientific Information: P10721 (http://www.expasy.org/uniprot/P10721) 




EGFR
(Epidermal growth factor receptor, Receptor tyrosine-protein kinase ErbB-1)

• CAT#: EGFR

• Enzyme: Human EGFR

• Assay methods: FRET; ATP 10 μM

• Inhibitor IC50 (nM):
  Staurosporine 127.6
  AG1478 0.33

• Scientific Information: P00533 (http://www.expasy.org/uniprot/P00533) 




EGFR (T790M)
(Epidermal growth factor receptor, Receptor tyrosine-protein kinase ErbB-1)

• CAT#: EGFR

• Enzyme: Human EGFR (T790M)

• Assay methods: FRET; ATP 10 μM

• Inhibitor IC50 (nM):
  Staurosporine 24.4
  AG1478 12.21

• Scientific Information: P00533 (http://www.expasy.org/uniprot/P00533) 




MMP1
(MMP1)

• CAT#: MMP1

• Enzyme: Recombinant Human MMP1 catalytic domain

• Assay methods: FRET， substrate, MCA-pro-leu-Gly-DPa-Ala-Arg-NH2.AcOH, 5 uM.

• Inhibitor IC50 (nM)
  GM6001， 659.2 




ADAM10
Recombinant Human ADAM10

• CAT#: ADAM10

• Enzyme: Human ADAM10

• Assay methods: Fluorogenic Peptide substrate: MCA-lys-pro-leu-Gly-leu-DPA-Ala-Arg-NH2, 10 uM

• Inhibitor IC50 (nM)
  GM6001， 175.3

 


DPP4
(Proto-oncogene tyrosine-protein kinase ABL1, c-ABL, p150, Abelson murine leukemia viral oncogene homolog 1)

• CAT#: ABL1

• Enzyme: Human ABL1

• Assay methods: Fluorogenic Substrate GP-AMC, 25μM.

• Inhibitor IC50 (nM)
  SYR0322，3.4
  BI-1356，0.3

• Scientific Information: 




HCV-NS3/4A1
• CAT#: HCV-NS3/4A1

• Enzyme: HCV-NS3/4A1

• Assay methods: FRET;

• Inhibitor IC50 (nM)
  AG ， 680.3 




HDAC1
(Histone deacetylase 1, Class I)

• CAT#: HDAC1

• Enzyme: Human HDAC1

• Substrate: Fluorogenic peptide from p53 residues 379-382 (RHKKAc), 50 uM

• Reference Compound IC50s:

Inhibitors IC50 (nM)
Trichostatin A 6.342
SAHA 138

• Scientific Information: Q13547 (http://www.expasy.org/uniprot/Q13547) 




HDAC-7
(Histone deacetylase 7a, HDAC7A, Class IIa)

• CAT#: HDAC7

• Enzyme: Human HDAC7

• Substrate: Fluorogenic HDAC Class2a Substrate (Boc-Lys(trifluoroacetyl)-AMC), 2 uM

• Reference Compound IC50s:

Compounds IC50 (nM)
Trichostatin A 855.5
SAHA 105,000

• Scientific Information: Q8WUI4 (http://www.expasy.org/uniprot/Q8WUI4) 




Influenza H1N1 Cell-Based Assay

• CAT#: H1N1-cell-viability-assay

• Cell line: MDCK

• Assay methods: Cell viability MTT assay

• Inhibitor IC50 (nM)
  RIBA， 53840
  OSE， 2.11
  Nucleozin， 330.9 



Influenza H3N2 Cell-Based Assay

• CAT#: H3N2-cell-viability-assay

• Cell line: MDCK

• Assay methods: Cell viability MTT assay

• Inhibitor IC50 (nM)
  AMD， 410.5
  OSE， 1.65
  Nucleozin， 556.5 




Influenza H1N1 Plaque assay

• CAT#: H1N1 Plaque assay

• Cell line: MDCK

• Assay methods: Plaque assay

• Inhibitor IC50 (nM)
  RIBA， 41520 




Influenza H1N1 Neuraminidase Assay

• CAT#: H1N1 Neuraminidase Assay

• Enzyme: H1N1 Neuraminidase

• Assay methods: substrate

• Inhibitor IC50 (nM)
  OSE， 95.37 




Influenza H3N2 Neuraminidase Assay

• CAT#: H3N2 Neuraminidase Assay

• Enzyme: H3N2 Neuraminidase

• Assay methods: substrate

• Inhibitor IC50 (nM)
  OSE， 0.42 




CYP450 1A2 Assay

• CAT#: CYP450-1A2 Assay

• Enzyme: CYP450-2A1

• Assay methods: substrate

• Inhibitor IC50 (uM)
  Ketoconazole， 25.44 




CYP450 2C9 Assay

• CAT#: CYP450-2C9 Assay

• Enzyme: CYP450-2C9

• Assay methods: substrate

• Inhibitor IC50 (uM)
  Ketoconazole， 2.63 




CYP450 2C19 Assay

• CAT#: CYP450-2C19 Assay

• Enzyme: CYP450-2C19

• Assay methods: substrate

• Inhibitor IC50 (uM)
  Ketoconazole， 2.75 




CYP450 2D6 Assay

• CAT#: CYP450-2D6Assay

• Enzyme: CYP450-2D6

• Assay methods: substrate

• Inhibitor IC50 (uM)
  Ketoconazole， 3.00 




CYP450 3A4 Assay

• CAT#: CYP450-3A4Assay

• Enzyme: CYP450-3A4

• Assay methods: substrate

• Inhibitor IC50 (nM)
  Ketoconazole，37.54