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Assay Detail

CHEMBL3636740

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

Binding
Inhibition of Pim1 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins
39
Total Activities
39
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

Target

Serine/threonine-protein kinase pim-1 (CHEMBL2147)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.
Hu H, Wang X, Chan GK, Chang JH, Do S, Drummond J, Ebens A, Lee W, Ly J, Lyssikatos JP, Murray J, Moffat JG, Chao Q, Tsui V, Wallweber H, Kolesnikov A.
Bioorg Med Chem Lett (2015) 25 : 5258 -5264
PubMed 26459208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 8.71 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3634783 1 11.00
CHEMBL3634760 1 10.89
CHEMBL3634769 1 10.82
CHEMBL3634767 1 10.70
CHEMBL3634772 1 10.68
CHEMBL3634771 1 10.66
CHEMBL3634757 1 10.46
CHEMBL3634770 1 10.44
CHEMBL3634781 1 10.40
CHEMBL3634782 1 10.39
CHEMBL3634758 1 10.22
CHEMBL3634761 1 10.14
CHEMBL3634779 1 10.00
CHEMBL3634756 1 9.85
CHEMBL3634768 1 9.66
CHEMBL3634755 1 9.57
CHEMBL3634780 1 9.52
CHEMBL3634759 1 9.41
CHEMBL3634773 1 8.74
CHEMBL3634775 1 8.70
CHEMBL3634765 1 8.48
CHEMBL3634777 1 8.47
CHEMBL3634763 1 8.40
CHEMBL3634778 1 8.22
CHEMBL3634766 1 8.11
CHEMBL3634762 1 8.07
CHEMBL3634790 1 8.00
CHEMBL3634791 1 8.00
CHEMBL3634764 1 7.89
CHEMBL3634793 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3634783 Ki = 0.01 nM 11.00
CHEMBL3634760 Ki = 0.013 nM 10.89
CHEMBL3634769 Ki = 0.015 nM 10.82
CHEMBL3634767 Ki = 0.02 nM 10.70
CHEMBL3634772 Ki = 0.021 nM 10.68
CHEMBL3634771 Ki = 0.022 nM 10.66
CHEMBL3634757 Ki = 0.035 nM 10.46
CHEMBL3634770 Ki = 0.036 nM 10.44
CHEMBL3634781 Ki = 0.04 nM 10.40
CHEMBL3634782 Ki = 0.041 nM 10.39
CHEMBL3634758 Ki = 0.06 nM 10.22
CHEMBL3634761 Ki = 0.073 nM 10.14
CHEMBL3634779 Ki = 0.1 nM 10.00
CHEMBL3634756 Ki = 0.14 nM 9.85
CHEMBL3634768 Ki = 0.22 nM 9.66
CHEMBL3634755 Ki = 0.27 nM 9.57
CHEMBL3634780 Ki = 0.3 nM 9.52
CHEMBL3634759 Ki = 0.39 nM 9.41
CHEMBL3634773 Ki = 1.82 nM 8.74
CHEMBL3634775 Ki = 2.0 nM 8.70
CHEMBL3634765 Ki = 3.3 nM 8.48
CHEMBL3634777 Ki = 3.4 nM 8.47
CHEMBL3634763 Ki = 4.0 nM 8.40
CHEMBL3634778 Ki = 6.0 nM 8.22
CHEMBL3634766 Ki = 7.7 nM 8.11
CHEMBL3634762 Ki = 8.5 nM 8.07
CHEMBL3634790 Ki = 10.0 nM 8.00
CHEMBL3634791 Ki = 10.0 nM 8.00
CHEMBL3634764 Ki = 13.0 nM 7.89
CHEMBL3634793 Ki = 14.0 nM 7.85
CHEMBL3634776 Ki = 31.0 nM 7.51
CHEMBL3634774 Ki = 171.0 nM 6.77
CHEMBL3634786 Ki = 200.0 nM 6.70
CHEMBL3634788 Ki = 300.0 nM 6.52
CHEMBL3634787 Ki = 800.0 nM 6.10
CHEMBL3634784 Ki = 1300.0 nM 5.89
CHEMBL3634789 Ki = 3200.0 nM 5.50
CHEMBL3634785 Ki = 3300.0 nM 5.48
CHEMBL3634792 Ki = 3500.0 nM 5.46