Literature summary for 3.1.4.53 extracted from

Card, G.L.; Blasdel, L.; England, B.P.; Zhang, C.; Suzuki, Y.; Gillette, S.; Fong, D.; Ibrahim, P.N.; Artis, D.R.; Bollag, G.; Milburn, M.V.; Kim, S.H.; Schlessinger, J.; Zhang, K.Y.
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design (2005), Nat. Biotechnol., 23, 201-207.

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Inhibitors

Inhibitors	Comment	Organism	Structure
ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate	IC50: 0.00027 mM, PDE4D; IC50: 0.00031 mM, PDE4B	Homo sapiens
ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate	IC50: 0.017 mM, PDE4B; IC50: 0.019 mM, PDE4D	Homo sapiens
ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate	IC50: 0.015 mM, PDE4B; IC50: 0.019 mM, PDE4D	Homo sapiens
ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate	IC50: 0.00088 mM, PDE4D; IC50: 0.0015 mM, PDE4B	Homo sapiens
ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate	IC50: 0.06 mM, PDE4B; IC50: 0.082 mM, PDE4D	Homo sapiens
ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate	IC50: 0.025 mM, PDE4B; IC50: 0.05 mM, PDE4D	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Synonyms

Synonyms	Comment	Organism
PDE4B	-	Homo sapiens
PDE4D	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00027	-	IC50: 0.00027 mM, PDE4D	Homo sapiens	ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
0.00031	-	IC50: 0.00031 mM, PDE4B	Homo sapiens	ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
0.00088	-	IC50: 0.00088 mM, PDE4D	Homo sapiens	ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
0.0015	-	IC50: 0.0015 mM, PDE4B	Homo sapiens	ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
0.015	-	IC50: 0.015 mM, PDE4B	Homo sapiens	ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
0.017	-	IC50: 0.017 mM, PDE4B	Homo sapiens	ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
0.019	-	IC50: 0.019 mM, PDE4D	Homo sapiens	ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
0.019	-	IC50: 0.019 mM, PDE4D	Homo sapiens	ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
0.025	-	IC50: 0.025 mM, PDE4B	Homo sapiens	ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
0.05	-	IC50: 0.05 mM, PDE4D	Homo sapiens	ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
0.06	-	IC50: 0.06 mM, PDE4B	Homo sapiens	ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate
0.082	-	IC50: 0.082 mM, PDE4D	Homo sapiens	ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate

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Release 2023.1 (January 2023)