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Assay Detail

CHEMBL2422528

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Binding
Inhibition of PDE10A (unknown origin)
29
Total Activities
29
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

Publication

N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
Kilburn JP, Kehler J, Langgård M, Erichsen MN, Leth-Petersen S, Larsen M, Christoffersen CT, Nielsen J.
Bioorg Med Chem (2013) 21 : 6053 -6062
PubMed 23978358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.88 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL562318 MARDEPODECT 2.0 1 8.59
CHEMBL2419369 1 7.92
CHEMBL2419368 1 7.89
CHEMBL2419555 1 7.80
CHEMBL2419366 1 7.62
CHEMBL2419561 1 7.51
CHEMBL1086110 1 7.50
CHEMBL2419548 1 7.21
CHEMBL219445 1 7.19
CHEMBL2419364 1 7.06
CHEMBL2419365 1 7.06
CHEMBL2419554 1 7.03
CHEMBL2419367 1 6.96
CHEMBL2419553 1 6.89
CHEMBL2419552 1 6.85
CHEMBL19224 PAPAVERINE 3.0 1 6.68
CHEMBL2419551 1 6.62
CHEMBL2419564 1 6.60
CHEMBL2419550 1 6.40
CHEMBL2419560 1 6.34
CHEMBL2419557 1 6.18
CHEMBL2419556 1 6.18
CHEMBL2419563 1 6.12
CHEMBL2419547 1 6.04
CHEMBL2419549 1 6.02
CHEMBL2419371 1 5.80
CHEMBL2419370 1 5.80
CHEMBL2419559 1 -
CHEMBL2419558 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL562318 MARDEPODECT IC50 = 2.6 nM 8.59
CHEMBL2419369 IC50 = 12.0 nM 7.92
CHEMBL2419368 IC50 = 13.0 nM 7.89
CHEMBL2419555 IC50 = 16.0 nM 7.80
CHEMBL2419366 IC50 = 24.0 nM 7.62
CHEMBL2419561 IC50 = 31.0 nM 7.51
CHEMBL1086110 IC50 = 32.0 nM 7.50
CHEMBL2419548 IC50 = 61.0 nM 7.21
CHEMBL219445 IC50 = 64.0 nM 7.19
CHEMBL2419364 IC50 = 88.0 nM 7.06
CHEMBL2419365 IC50 = 87.0 nM 7.06
CHEMBL2419554 IC50 = 93.0 nM 7.03
CHEMBL2419367 IC50 = 110.0 nM 6.96
CHEMBL2419553 IC50 = 130.0 nM 6.89
CHEMBL2419552 IC50 = 140.0 nM 6.85
CHEMBL19224 PAPAVERINE IC50 = 210.0 nM 6.68
CHEMBL2419551 IC50 = 240.0 nM 6.62
CHEMBL2419564 IC50 = 250.0 nM 6.60
CHEMBL2419550 IC50 = 400.0 nM 6.40
CHEMBL2419560 IC50 = 460.0 nM 6.34
CHEMBL2419557 IC50 = 660.0 nM 6.18
CHEMBL2419556 IC50 = 660.0 nM 6.18
CHEMBL2419563 IC50 = 750.0 nM 6.12
CHEMBL2419547 IC50 = 920.0 nM 6.04
CHEMBL2419549 IC50 = 950.0 nM 6.02
CHEMBL2419371 IC50 = 1600.0 nM 5.80
CHEMBL2419370 IC50 = 1600.0 nM 5.80
CHEMBL2419559 IC50 - -
CHEMBL2419558 IC50 - -