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Assay Detail

CHEMBL2174779

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

Binding
Inhibition of cloned human recombinant PDE7A assessed as [3H]cAMP hydrolysis by radiometric assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (CHEMBL3012)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazopyridazinones as novel PDE7 inhibitors: SAR and in vivo studies in Parkinson's disease model.
Banerjee A, Patil S, Pawar MY, Gullapalli S, Gupta PK, Gandhi MN, Bhateja DK, Bajpai M, Sangana RR, Gudi GS, Khairatkar-Joshi N, Gharat LA.
Bioorg Med Chem Lett (2012) 22 : 6286 -6291
PubMed 22944118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.37 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2171440 1 8.52
CHEMBL2171423 1 7.92
CHEMBL2171435 1 7.75
CHEMBL2171436 1 7.62
CHEMBL2171422 1 7.57
CHEMBL2171421 1 7.51
CHEMBL2171434 1 7.50
CHEMBL2171433 1 7.48
CHEMBL2171429 1 7.35
CHEMBL2171430 1 7.28
CHEMBL2171428 1 7.26
CHEMBL2171437 1 7.17
CHEMBL2171431 1 7.15
CHEMBL2171427 1 7.14
CHEMBL2171442 1 7.12
CHEMBL2171426 1 7.11
CHEMBL2171425 1 7.10
CHEMBL2171432 1 7.09
CHEMBL2171438 1 7.05
CHEMBL2171439 1 7.03
CHEMBL2171424 1 6.98
CHEMBL2171441 1 -
CHEMBL2171443 1 -
CHEMBL2171444 1 -
CHEMBL2171445 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2171440 IC50 = 3.0 nM 8.52
CHEMBL2171423 IC50 = 12.0 nM 7.92
CHEMBL2171435 IC50 = 18.0 nM 7.75
CHEMBL2171436 IC50 = 24.0 nM 7.62
CHEMBL2171422 IC50 = 27.0 nM 7.57
CHEMBL2171421 IC50 = 31.0 nM 7.51
CHEMBL2171434 IC50 = 32.0 nM 7.50
CHEMBL2171433 IC50 = 33.0 nM 7.48
CHEMBL2171429 IC50 = 45.0 nM 7.35
CHEMBL2171430 IC50 = 53.0 nM 7.28
CHEMBL2171428 IC50 = 55.0 nM 7.26
CHEMBL2171437 IC50 = 68.0 nM 7.17
CHEMBL2171431 IC50 = 71.0 nM 7.15
CHEMBL2171427 IC50 = 73.0 nM 7.14
CHEMBL2171442 IC50 = 75.0 nM 7.12
CHEMBL2171426 IC50 = 77.0 nM 7.11
CHEMBL2171425 IC50 = 80.0 nM 7.10
CHEMBL2171432 IC50 = 81.0 nM 7.09
CHEMBL2171438 IC50 = 89.0 nM 7.05
CHEMBL2171439 IC50 = 93.0 nM 7.03
CHEMBL2171424 IC50 = 104.0 nM 6.98
CHEMBL2171441 IC50 - -
CHEMBL2171443 IC50 - -
CHEMBL2171444 IC50 - -
CHEMBL2171445 IC50 - -