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Assay Detail

CHEMBL2071880

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

Binding
Inhibition of human recombinant PDE10A-catalyzed cAMP hydrolysis
42
Total Activities
42
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

Novel triazines as potent and selective phosphodiesterase 10A inhibitors.
Malamas MS, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Hage T, Ni Y, Erdei J, Fan KY, Parris K, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Brandon NJ, Hoefgen N.
Bioorg Med Chem Lett (2012) 22 : 5876 -5884
PubMed 22902656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 8.00 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2069321 1 9.55
CHEMBL2070655 1 9.07
CHEMBL2070651 1 8.83
CHEMBL2070666 1 8.83
CHEMBL2070654 1 8.81
CHEMBL2070664 1 8.78
CHEMBL2070668 1 8.73
CHEMBL2070653 1 8.69
CHEMBL2070648 1 8.62
CHEMBL2070647 1 8.48
CHEMBL2070650 1 8.47
CHEMBL2070659 1 8.45
CHEMBL2070656 1 8.40
CHEMBL2070652 1 8.38
CHEMBL2070667 1 8.29
CHEMBL2070649 1 8.29
CHEMBL2070657 1 8.19
CHEMBL2070669 1 8.15
CHEMBL2070661 1 8.14
CHEMBL2070662 1 8.11
CHEMBL2070670 1 8.08
CHEMBL2070658 1 8.04
CHEMBL2070671 1 8.03
CHEMBL2070641 1 8.01
CHEMBL2070645 1 8.00
CHEMBL2070665 1 7.93
CHEMBL2070646 1 7.91
CHEMBL2070639 1 7.88
CHEMBL2070663 1 7.88
CHEMBL2070631 1 7.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2069321 IC50 = 0.28 nM 9.55
CHEMBL2070655 IC50 = 0.85 nM 9.07
CHEMBL2070666 IC50 = 1.48 nM 8.83
CHEMBL2070651 IC50 = 1.48 nM 8.83
CHEMBL2070654 IC50 = 1.53 nM 8.81
CHEMBL2070664 IC50 = 1.65 nM 8.78
CHEMBL2070668 IC50 = 1.85 nM 8.73
CHEMBL2070653 IC50 = 2.06 nM 8.69
CHEMBL2070648 IC50 = 2.41 nM 8.62
CHEMBL2070647 IC50 = 3.3 nM 8.48
CHEMBL2070650 IC50 = 3.35 nM 8.47
CHEMBL2070659 IC50 = 3.55 nM 8.45
CHEMBL2070656 IC50 = 3.99 nM 8.40
CHEMBL2070652 IC50 = 4.16 nM 8.38
CHEMBL2070649 IC50 = 5.13 nM 8.29
CHEMBL2070667 IC50 = 5.11 nM 8.29
CHEMBL2070657 IC50 = 6.53 nM 8.19
CHEMBL2070669 IC50 = 7.0 nM 8.15
CHEMBL2070661 IC50 = 7.2 nM 8.14
CHEMBL2070662 IC50 = 7.84 nM 8.11
CHEMBL2070670 IC50 = 8.33 nM 8.08
CHEMBL2070658 IC50 = 9.11 nM 8.04
CHEMBL2070671 IC50 = 9.43 nM 8.03
CHEMBL2070641 IC50 = 9.83 nM 8.01
CHEMBL2070645 IC50 = 10.1 nM 8.00
CHEMBL2070665 IC50 = 11.7 nM 7.93
CHEMBL2070646 IC50 = 12.4 nM 7.91
CHEMBL2070639 IC50 = 13.1 nM 7.88
CHEMBL2070663 IC50 = 13.1 nM 7.88
CHEMBL2070631 IC50 = 13.1 nM 7.88
CHEMBL2070640 IC50 = 15.0 nM 7.82
CHEMBL2070660 IC50 = 25.4 nM 7.59
CHEMBL2070644 IC50 = 42.4 nM 7.37
CHEMBL2070633 IC50 = 45.9 nM 7.34
CHEMBL2070634 IC50 = 47.6 nM 7.32
CHEMBL2070637 IC50 = 51.5 nM 7.29
CHEMBL2070632 IC50 = 53.1 nM 7.28
CHEMBL2070635 IC50 = 64.5 nM 7.19
CHEMBL2070636 IC50 = 91.3 nM 7.04
CHEMBL2070642 IC50 = 114.0 nM 6.94
CHEMBL2070638 IC50 = 388.0 nM 6.41
CHEMBL2070643 IC50 = 2430.0 nM 5.61