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Assay Detail

CHEMBL1768778

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Binding
Inhibition of PDK1
ChEMBL ↗
50
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Medina JR, Becker CJ, Blackledge CW, Duquenne C, Feng Y, Grant SW, Heerding D, Li WH, Miller WH, Romeril SP, Scherzer D, Shu A, Bobko MA, Chadderton AR, Dumble M, Gardiner CM, Gilbert S, Liu Q, Rabindran SK, Sudakin V, Xiang H, Brady PG, Campobasso N, Ward P, Axten JM.
J Med Chem (2011) 54 : 1871 -1895
PubMed 21341675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 7.14 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1765751 — — 1 9.20
CHEMBL1765750 — — 1 9.10
CHEMBL1765738 — — 1 8.80
CHEMBL1765740 — — 2 8.60
CHEMBL1765743 — — 1 8.50
CHEMBL1765742 — — 1 8.50
CHEMBL1614775 — — 1 8.50
CHEMBL1765741 — — 1 8.30
CHEMBL1765744 — — 1 8.20
CHEMBL1614777 — — 1 8.20
CHEMBL1765739 — — 1 8.10
CHEMBL1614776 — — 2 8.00
CHEMBL1765876 — — 1 7.70
CHEMBL1614774 — — 1 7.70
CHEMBL1765748 — — 1 7.60
CHEMBL1765732 — — 1 7.50
CHEMBL1765728 — — 1 7.50
CHEMBL1765746 — — 1 7.30
CHEMBL1765762 — — 1 7.30
CHEMBL1765745 — — 1 7.20
CHEMBL1614773 — — 1 7.20
CHEMBL1765734 — — 1 7.20
CHEMBL1765760 — — 1 7.10
CHEMBL1765735 — — 1 6.90
CHEMBL1765761 — — 1 6.90
CHEMBL1765733 — — 1 6.90
CHEMBL1765730 — — 1 6.90
CHEMBL1765756 — — 1 6.90
CHEMBL1614771 — — 1 6.80
CHEMBL1765729 — — 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1765751 — IC50 = 0.631 nM 9.20
CHEMBL1765750 — IC50 = 0.7943 nM 9.10
CHEMBL1765738 — IC50 = 1.585 nM 8.80
CHEMBL1765740 — IC50 = 2.5 nM 8.60
CHEMBL1765740 — IC50 = 2.512 nM 8.60
CHEMBL1765743 — IC50 = 3.162 nM 8.50
CHEMBL1765742 — IC50 = 3.162 nM 8.50
CHEMBL1614775 — IC50 = 3.162 nM 8.50
CHEMBL1765741 — IC50 = 5.012 nM 8.30
CHEMBL1614777 — IC50 = 6.31 nM 8.20
CHEMBL1765744 — IC50 = 6.31 nM 8.20
CHEMBL1765739 — IC50 = 7.943 nM 8.10
CHEMBL1614776 — IC50 = 10.0 nM 8.00
CHEMBL1614776 — IC50 = 15.85 nM 7.80
CHEMBL1765876 — IC50 = 19.95 nM 7.70
CHEMBL1614774 — IC50 = 19.95 nM 7.70
CHEMBL1765748 — IC50 = 25.12 nM 7.60
CHEMBL1765728 — IC50 = 31.62 nM 7.50
CHEMBL1765732 — IC50 = 31.62 nM 7.50
CHEMBL1765762 — IC50 = 50.12 nM 7.30
CHEMBL1765746 — IC50 = 50.12 nM 7.30
CHEMBL1765745 — IC50 = 63.1 nM 7.20
CHEMBL1765734 — IC50 = 63.1 nM 7.20
CHEMBL1614773 — IC50 = 63.1 nM 7.20
CHEMBL1765760 — IC50 = 79.43 nM 7.10
CHEMBL1765733 — IC50 = 125.89 nM 6.90
CHEMBL1765730 — IC50 = 125.89 nM 6.90
CHEMBL1765735 — IC50 = 125.89 nM 6.90
CHEMBL1765761 — IC50 = 125.89 nM 6.90
CHEMBL1765756 — IC50 = 125.89 nM 6.90
CHEMBL1614771 — IC50 = 158.49 nM 6.80
CHEMBL1765729 — IC50 = 199.53 nM 6.70
CHEMBL1765758 — IC50 = 199.53 nM 6.70
CHEMBL1765759 — IC50 = 251.19 nM 6.60
CHEMBL1765879 — IC50 = 251.19 nM 6.60
CHEMBL1765878 — IC50 = 251.19 nM 6.60
CHEMBL1765757 — IC50 = 251.19 nM 6.60
CHEMBL1614772 — IC50 = 316.23 nM 6.50
CHEMBL1688215 — IC50 = 398.11 nM 6.40
CHEMBL1765877 — IC50 = 501.19 nM 6.30
CHEMBL1765749 — IC50 = 630.96 nM 6.20
CHEMBL1765737 — IC50 = 794.33 nM 6.10
CHEMBL1765752 — IC50 = 1000.0 nM 6.00
CHEMBL1765747 — IC50 = 1000.0 nM 6.00
CHEMBL1765731 — IC50 = 1000.0 nM 6.00
CHEMBL1765727 — IC50 = 1258.93 nM 5.90
CHEMBL1765736 — IC50 = 1258.93 nM 5.90
CHEMBL1765754 — IC50 = 7943.28 nM 5.10
CHEMBL1765755 — IC50 = 12589.25 nM 4.90
CHEMBL1765753 — IC50 = 19952.62 nM 4.70