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Assay Detail

CHEMBL4122466

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

Binding
Inhibition of full length recombinant human PDE1B1 using 3',5'-[3H]cAMP as substrate after 30 mins by scintillation proximity assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Publication

Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.
Humphrey JM, Movsesian M, Am Ende CW, Becker SL, Chappie TA, Jenkinson S, Liras JL, Liras S, Orozco C, Pandit J, Vajdos FF, Vandeput F, Yang E, Menniti FS.
J Med Chem (2018) 61 : 4635 -4640
PubMed 29718668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.51 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4126270 1 8.35
CHEMBL4128481 1 8.04
CHEMBL4127641 1 7.68
CHEMBL4128897 1 7.57
CHEMBL3601554 1 7.46
CHEMBL4127499 1 7.28
CHEMBL4129844 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4126270 IC50 = 4.5 nM 8.35
CHEMBL4128481 IC50 = 9.1 nM 8.04
CHEMBL4127641 IC50 = 21.0 nM 7.68
CHEMBL4128897 IC50 = 27.0 nM 7.57
CHEMBL3601554 IC50 = 35.0 nM 7.46
CHEMBL4127499 IC50 = 52.0 nM 7.28
CHEMBL4129844 IC50 = 596.0 nM 6.22