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Assay Detail

CHEMBL1068541

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Binding
Inhibition of bovine retina PDE6
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of potent, selective, and orally bioavailable PDE5 inhibitor: Methyl-4-(3-chloro-4-methoxybenzylamino)-8-(2-hydroxyethyl)-7-methoxyquinazolin-6-ylmethylcarbamate (CKD 533).
Choi H, Lee J, Kim YH, Im DS, Hwang IC, Kim SJ, Moon SK, Lee HW, Lee SS, Ahn SK, Kim SW, Choi NS, Lee KJ.
Bioorg Med Chem Lett (2010) 20 : 383 -386
PubMed 19906530 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.20 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL594160 1 6.85
CHEMBL192 SILDENAFIL 4.0 1 6.85
CHEMBL604271 1 6.50
CHEMBL595104 1 6.47
CHEMBL521075 1 6.34
CHEMBL596489 1 6.22
CHEMBL603422 1 6.15
CHEMBL592986 1 5.96
CHEMBL779 TADALAFIL 4.0 1 5.52
CHEMBL593225 1 5.10
CHEMBL595330 1 -
CHEMBL596454 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL594160 IC50 = 140.0 nM 6.85
CHEMBL192 SILDENAFIL IC50 = 140.0 nM 6.85
CHEMBL604271 IC50 = 320.0 nM 6.50
CHEMBL595104 IC50 = 340.0 nM 6.47
CHEMBL521075 IC50 = 460.0 nM 6.34
CHEMBL596489 IC50 = 600.0 nM 6.22
CHEMBL603422 IC50 = 710.0 nM 6.15
CHEMBL592986 IC50 = 1100.0 nM 5.96
CHEMBL779 TADALAFIL IC50 = 3000.0 nM 5.52
CHEMBL593225 IC50 = 7950.0 nM 5.10
CHEMBL595330 IC50 - -
CHEMBL596454 IC50 - -