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Assay Detail

CHEMBL763643

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

Binding
Binding affinity towards rolipram binding site on phosphodiesterase 4 using [3H]rolipram as radioligand in crude rat brain homogenate
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2094267)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
Kim E, Chun HO, Jung SH, Kim JH, Lee JM, Suh BC, Xiang MX, Rhee CK.
Bioorg Med Chem Lett (2003) 13 : 2355 -2358
PubMed 12824033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 9.46 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77788 1 10.72
CHEMBL75684 1 10.38
CHEMBL76382 1 10.34
CHEMBL432348 1 10.16
CHEMBL78237 1 10.04
CHEMBL77358 1 9.84
CHEMBL77745 1 9.47
CHEMBL76635 1 8.92
CHEMBL77999 1 8.81
CHEMBL76257 1 8.70
CHEMBL78238 1 8.64
CHEMBL80258 1 8.56
CHEMBL306320 1 8.46
CHEMBL77177 1 -
CHEMBL63 ROLIPRAM 2.0 1 -
CHEMBL431962 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77788 Ki = 0.019 nM 10.72
CHEMBL75684 Ki = 0.042 nM 10.38
CHEMBL76382 Ki = 0.046 nM 10.34
CHEMBL432348 Ki = 0.069 nM 10.16
CHEMBL78237 Ki = 0.092 nM 10.04
CHEMBL77358 Ki = 0.146 nM 9.84
CHEMBL77745 Ki = 0.336 nM 9.47
CHEMBL76635 Ki = 1.197 nM 8.92
CHEMBL77999 Ki = 1.559 nM 8.81
CHEMBL76257 Ki = 2.02 nM 8.70
CHEMBL78238 Ki = 2.31 nM 8.64
CHEMBL80258 Ki = 2.73 nM 8.56
CHEMBL306320 Ki = 3.455 nM 8.46
CHEMBL77177 Ki > 5.0 nM -
CHEMBL63 ROLIPRAM Ki = 0.0023 nM -
CHEMBL431962 Ki > 5.0 nM -