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Assay Detail

CHEMBL2045987

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

Binding
Inhibition of PHD1
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prolyl hydroxylase EGLN2 (CHEMBL3028) ↗
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 56 9.01 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2041182 — — 1 9.70
CHEMBL2041185 — — 1 9.70
CHEMBL2043325 — — 1 9.70
CHEMBL2043169 — — 1 9.70
CHEMBL2041190 — — 1 9.70
CHEMBL2041175 — — 1 9.70
CHEMBL2041193 — — 1 9.70
CHEMBL2041169 — — 1 9.70
CHEMBL2043168 — — 1 9.52
CHEMBL2041192 — — 1 9.52
CHEMBL2041178 — — 1 9.52
CHEMBL2041188 — — 1 9.52
CHEMBL2041184 — — 1 9.52
CHEMBL2041010 — — 1 9.52
CHEMBL2043326 — — 1 9.52
CHEMBL2041186 — — 1 9.52
CHEMBL2043324 — — 1 9.40
CHEMBL2041189 — — 1 9.40
CHEMBL2040897 — — 1 9.40
CHEMBL2041183 — — 1 9.40
CHEMBL2041170 — — 1 9.30
CHEMBL2040854 — — 1 9.30
CHEMBL2041177 — — 1 9.15
CHEMBL2041164 — — 1 9.10
CHEMBL2041171 — — 1 9.10
CHEMBL2043171 — — 1 9.05
CHEMBL2041194 — — 1 9.00
CHEMBL2041191 — — 1 9.00
CHEMBL2041180 — — 1 8.96
CHEMBL2043011 — — 1 8.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2041182 — IC50 = 0.2 nM 9.70
CHEMBL2041169 — IC50 = 0.2 nM 9.70
CHEMBL2041193 — IC50 = 0.2 nM 9.70
CHEMBL2041175 — IC50 = 0.2 nM 9.70
CHEMBL2041190 — IC50 = 0.2 nM 9.70
CHEMBL2043325 — IC50 = 0.2 nM 9.70
CHEMBL2041185 — IC50 = 0.2 nM 9.70
CHEMBL2043169 — IC50 = 0.2 nM 9.70
CHEMBL2043168 — IC50 = 0.3 nM 9.52
CHEMBL2041192 — IC50 = 0.3 nM 9.52
CHEMBL2041178 — IC50 = 0.3 nM 9.52
CHEMBL2041188 — IC50 = 0.3 nM 9.52
CHEMBL2041186 — IC50 = 0.3 nM 9.52
CHEMBL2041184 — IC50 = 0.3 nM 9.52
CHEMBL2041010 — IC50 = 0.3 nM 9.52
CHEMBL2043326 — IC50 = 0.3 nM 9.52
CHEMBL2043324 — IC50 = 0.4 nM 9.40
CHEMBL2041189 — IC50 = 0.4 nM 9.40
CHEMBL2040897 — IC50 = 0.4 nM 9.40
CHEMBL2041183 — IC50 = 0.4 nM 9.40
CHEMBL2040854 — IC50 = 0.5 nM 9.30
CHEMBL2041170 — IC50 = 0.5 nM 9.30
CHEMBL2041177 — IC50 = 0.7 nM 9.15
CHEMBL2041164 — IC50 = 0.8 nM 9.10
CHEMBL2041171 — IC50 = 0.8 nM 9.10
CHEMBL2043171 — IC50 = 0.9 nM 9.05
CHEMBL2041191 — IC50 = 1.0 nM 9.00
CHEMBL2041194 — IC50 = 1.0 nM 9.00
CHEMBL2041180 — IC50 = 1.1 nM 8.96
CHEMBL2043011 — IC50 = 1.1 nM 8.96
CHEMBL2043010 — IC50 = 1.1 nM 8.96
CHEMBL2041176 — IC50 = 1.1 nM 8.96
CHEMBL2041187 — IC50 = 1.2 nM 8.92
CHEMBL2043172 — IC50 = 1.2 nM 8.92
CHEMBL2043004 — IC50 = 1.3 nM 8.89
CHEMBL2043003 — IC50 = 1.4 nM 8.85
CHEMBL2043006 — IC50 = 1.4 nM 8.85
CHEMBL2043007 — IC50 = 1.4 nM 8.85
CHEMBL2041181 — IC50 = 1.6 nM 8.80
CHEMBL2043005 — IC50 = 1.7 nM 8.77
CHEMBL2041174 — IC50 = 1.8 nM 8.74
CHEMBL2043002 — IC50 = 1.8 nM 8.74
CHEMBL2043327 — IC50 = 1.9 nM 8.72
CHEMBL2041167 — IC50 = 2.0 nM 8.70
CHEMBL2041172 — IC50 = 2.1 nM 8.68
CHEMBL2043008 — IC50 = 2.1 nM 8.68
CHEMBL2041173 — IC50 = 2.3 nM 8.64
CHEMBL2041179 — IC50 = 3.7 nM 8.43
CHEMBL2040896 — IC50 = 4.5 nM 8.35
CHEMBL2041165 — IC50 = 5.5 nM 8.26