Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4405034

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

ADMET
Inhibition of human PDE4D2 expressed in Escherichia coli BL21 (DE3) using cAMP as substrate by PDELight HTS cAMP phosphodiesterase Kit based
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lead Optimization of Phthalazinone Phosphodiesterase Inhibitors as Novel Antitrypanosomal Compounds.
Salado IG, Singh AK, Moreno-Cinos C, Sakaine G, Siderius M, Van der Veken P, Matheeussen A, van der Meer T, Sadek P, Gul S, Maes L, Sterk GJ, Leurs R, Brown D, Augustyns K.
J Med Chem (2020) 63 : 3485 -3507
PubMed 32196340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 9.23 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4566742 1 10.21
CHEMBL4435111 1 9.92
CHEMBL4441748 1 9.91
CHEMBL4453005 1 9.81
CHEMBL4524402 1 9.81
CHEMBL4441871 1 9.79
CHEMBL4461456 1 9.77
CHEMBL4589927 1 9.65
CHEMBL4592553 1 9.63
CHEMBL4530777 1 9.52
CHEMBL4444578 1 9.50
CHEMBL4473426 1 9.50
CHEMBL4460623 1 9.45
CHEMBL4591859 1 9.41
CHEMBL4522249 1 9.29
CHEMBL4454600 1 9.25
CHEMBL4466777 1 9.18
CHEMBL4472307 1 9.17
CHEMBL4461705 1 9.17
CHEMBL4465097 1 9.07
CHEMBL4452707 1 9.06
CHEMBL4461658 1 8.93
CHEMBL4533993 1 8.79
CHEMBL4575003 1 8.61
CHEMBL4472329 1 8.61
CHEMBL4466905 1 8.59
CHEMBL4462322 1 7.52
CHEMBL4451207 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4566742 Ki = 0.06166 nM 10.21
CHEMBL4435111 Ki = 0.1202 nM 9.92
CHEMBL4441748 Ki = 0.123 nM 9.91
CHEMBL4453005 Ki = 0.1549 nM 9.81
CHEMBL4524402 Ki = 0.1549 nM 9.81
CHEMBL4441871 Ki = 0.1622 nM 9.79
CHEMBL4461456 Ki = 0.1698 nM 9.77
CHEMBL4589927 Ki = 0.2239 nM 9.65
CHEMBL4592553 Ki = 0.2344 nM 9.63
CHEMBL4530777 Ki = 0.302 nM 9.52
CHEMBL4444578 Ki = 0.3162 nM 9.50
CHEMBL4473426 Ki = 0.3162 nM 9.50
CHEMBL4460623 Ki = 0.3548 nM 9.45
CHEMBL4591859 Ki = 0.389 nM 9.41
CHEMBL4522249 Ki = 0.5129 nM 9.29
CHEMBL4454600 Ki = 0.5623 nM 9.25
CHEMBL4466777 Ki = 0.6607 nM 9.18
CHEMBL4472307 Ki = 0.6761 nM 9.17
CHEMBL4461705 Ki = 0.6761 nM 9.17
CHEMBL4465097 Ki = 0.8511 nM 9.07
CHEMBL4452707 Ki = 0.871 nM 9.06
CHEMBL4461658 Ki = 1.175 nM 8.93
CHEMBL4533993 Ki = 1.622 nM 8.79
CHEMBL4575003 Ki = 2.455 nM 8.61
CHEMBL4472329 Ki = 2.455 nM 8.61
CHEMBL4466905 Ki = 2.57 nM 8.59
CHEMBL4462322 Ki = 30.2 nM 7.52
CHEMBL4451207 Ki = 63.1 nM 7.20