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Assay Detail

CHEMBL2045986

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

Binding
Inhibition of FLAG-tagged PHD2 expressed in baculovirus infected insect sf9 cells using biotinyl-DLDLEMLAPYIPMDDDFQL as substrate preincubated with compound for 30 mins measured after 2 hrs by time resolved fluorescence analysis
ChEMBL ↗
100
Total Activities
100
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Egl nine homolog 1 (CHEMBL5697) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.
Vachal P, Miao S, Pierce JM, Guiadeen D, Colandrea VJ, Wyvratt MJ, Salowe SP, Sonatore LM, Milligan JA, Hajdu R, Gollapudi A, Keohane CA, Lingham RB, Mandala SM, DeMartino JA, Tong X, Wolff M, Steinhuebel D, Kieczykowski GR, Fleitz FJ, Chapman K, Athanasopoulos J, Adam G, Akyuz CD, Jena DK, Lusen JW, Meng J, Stein BD, Xia L, Sherer EC, Hale JJ.
J Med Chem (2012) 55 : 2945 -2959
PubMed 22364528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 100 8.09 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2041192 — — 1 9.70
CHEMBL2041175 — — 1 9.70
CHEMBL2041190 — — 1 9.70
CHEMBL2041169 — — 1 9.70
CHEMBL2041182 — — 1 9.70
CHEMBL2043325 — — 1 9.70
CHEMBL2041186 — — 1 9.70
CHEMBL2041185 — — 1 9.70
CHEMBL2041184 — — 1 9.70
CHEMBL2041193 — — 1 9.70
CHEMBL2043169 — — 1 9.40
CHEMBL2041189 — — 1 9.40
CHEMBL2041188 — — 1 9.40
CHEMBL2043010 — — 1 9.40
CHEMBL2043324 — — 1 9.40
CHEMBL2043168 — — 1 9.40
CHEMBL2043326 — — 1 9.30
CHEMBL2041178 — — 1 9.30
CHEMBL2041183 — — 1 9.30
CHEMBL2041170 — — 1 9.22
CHEMBL2041010 — — 1 9.22
CHEMBL2040854 — — 1 9.22
CHEMBL2042993 — — 1 9.15
CHEMBL2041194 — — 1 9.10
CHEMBL2043171 — — 1 9.10
CHEMBL2041177 — — 1 9.10
CHEMBL2041187 — — 1 9.10
CHEMBL2040897 — — 1 9.05
CHEMBL2043172 — — 1 9.00
CHEMBL2041191 — — 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2041192 — IC50 = 0.2 nM 9.70
CHEMBL2041193 — IC50 = 0.2 nM 9.70
CHEMBL2041184 — IC50 = 0.2 nM 9.70
CHEMBL2041185 — IC50 = 0.2 nM 9.70
CHEMBL2041186 — IC50 = 0.2 nM 9.70
CHEMBL2043325 — IC50 = 0.2 nM 9.70
CHEMBL2041169 — IC50 = 0.2 nM 9.70
CHEMBL2041190 — IC50 = 0.2 nM 9.70
CHEMBL2041175 — IC50 = 0.2 nM 9.70
CHEMBL2041182 — IC50 = 0.2 nM 9.70
CHEMBL2043169 — IC50 = 0.4 nM 9.40
CHEMBL2041189 — IC50 = 0.4 nM 9.40
CHEMBL2041188 — IC50 = 0.4 nM 9.40
CHEMBL2043168 — IC50 = 0.4 nM 9.40
CHEMBL2043010 — IC50 = 0.4 nM 9.40
CHEMBL2043324 — IC50 = 0.4 nM 9.40
CHEMBL2043326 — IC50 = 0.5 nM 9.30
CHEMBL2041178 — IC50 = 0.5 nM 9.30
CHEMBL2041183 — IC50 = 0.5 nM 9.30
CHEMBL2040854 — IC50 = 0.6 nM 9.22
CHEMBL2041010 — IC50 = 0.6 nM 9.22
CHEMBL2041170 — IC50 = 0.6 nM 9.22
CHEMBL2042993 — IC50 = 0.7 nM 9.15
CHEMBL2041187 — IC50 = 0.8 nM 9.10
CHEMBL2041177 — IC50 = 0.8 nM 9.10
CHEMBL2041194 — IC50 = 0.8 nM 9.10
CHEMBL2043171 — IC50 = 0.8 nM 9.10
CHEMBL2040897 — IC50 = 0.9 nM 9.05
CHEMBL2043172 — IC50 = 1.0 nM 9.00
CHEMBL2041191 — IC50 = 1.0 nM 9.00
CHEMBL2043011 — IC50 = 1.1 nM 8.96
CHEMBL2041171 — IC50 = 1.1 nM 8.96
CHEMBL2041174 — IC50 = 1.5 nM 8.82
CHEMBL2042995 — IC50 = 1.6 nM 8.80
CHEMBL2041180 — IC50 = 1.6 nM 8.80
CHEMBL2041176 — IC50 = 1.6 nM 8.80
CHEMBL2041181 — IC50 = 1.9 nM 8.72
CHEMBL2041172 — IC50 = 2.0 nM 8.70
CHEMBL2043005 — IC50 = 2.1 nM 8.68
CHEMBL2042994 — IC50 = 2.1 nM 8.68
CHEMBL2041173 — IC50 = 2.3 nM 8.64
CHEMBL2043004 — IC50 = 2.5 nM 8.60
CHEMBL2041164 — IC50 = 2.8 nM 8.55
CHEMBL2043002 — IC50 = 3.0 nM 8.52
CHEMBL2043007 — IC50 = 3.4 nM 8.47
CHEMBL2042996 — IC50 = 3.8 nM 8.42
CHEMBL2041167 — IC50 = 3.9 nM 8.41
CHEMBL2042853 — IC50 = 4.0 nM 8.40
CHEMBL2043008 — IC50 = 4.1 nM 8.39
CHEMBL2042992 — IC50 = 4.1 nM 8.39