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Assay Detail

CHEMBL1786237

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

Binding
Inhibition of human Pim1 using 5-FAM-RSRHSSYPAGT-CONH2 as substrate after 45 mins by off-chip mobility shift method
33
Total Activities
33
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

The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.
Xiang Y, Hirth B, Asmussen G, Biemann HP, Bishop KA, Good A, Fitzgerald M, Gladysheva T, Jain A, Jancsics K, Liu J, Metz M, Papoulis A, Skerlj R, Stepp JD, Wei RR.
Bioorg Med Chem Lett (2011) 21 : 3050 -3056
PubMed 21507633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.30 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782530 1 9.00
CHEMBL1782531 1 7.72
CHEMBL1782521 1 7.70
CHEMBL1782524 1 7.40
CHEMBL1782522 1 7.29
CHEMBL1782516 1 7.28
CHEMBL1782526 1 7.26
CHEMBL1782518 1 7.22
CHEMBL1782520 1 7.15
CHEMBL1782513 1 6.92
CHEMBL1782525 1 6.82
CHEMBL1782514 1 6.70
CHEMBL1782515 1 6.68
CHEMBL1782527 1 6.66
CHEMBL1782509 1 6.42
CHEMBL1782517 1 6.35
CHEMBL1782512 1 6.34
CHEMBL1782528 1 6.01
CHEMBL1782511 1 5.72
CHEMBL1782532 1 5.64
CHEMBL1782533 1 5.62
CHEMBL1782529 1 5.57
CHEMBL1782523 1 5.35
CHEMBL1782519 1 5.31
CHEMBL1782505 1 5.28
CHEMBL1782508 1 5.27
CHEMBL1738915 1 5.24
CHEMBL1782510 1 5.22
CHEMBL1782506 1 5.21
CHEMBL1782507 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782530 IC50 = 1.0 nM 9.00
CHEMBL1782531 IC50 = 19.0 nM 7.72
CHEMBL1782521 IC50 = 20.0 nM 7.70
CHEMBL1782524 IC50 = 40.0 nM 7.40
CHEMBL1782522 IC50 = 51.0 nM 7.29
CHEMBL1782516 IC50 = 53.0 nM 7.28
CHEMBL1782526 IC50 = 55.0 nM 7.26
CHEMBL1782518 IC50 = 60.0 nM 7.22
CHEMBL1782520 IC50 = 71.0 nM 7.15
CHEMBL1782513 IC50 = 120.0 nM 6.92
CHEMBL1782525 IC50 = 150.0 nM 6.82
CHEMBL1782514 IC50 = 200.0 nM 6.70
CHEMBL1782515 IC50 = 210.0 nM 6.68
CHEMBL1782527 IC50 = 220.0 nM 6.66
CHEMBL1782509 IC50 = 380.0 nM 6.42
CHEMBL1782517 IC50 = 450.0 nM 6.35
CHEMBL1782512 IC50 = 460.0 nM 6.34
CHEMBL1782528 IC50 = 980.0 nM 6.01
CHEMBL1782511 IC50 = 1900.0 nM 5.72
CHEMBL1782532 IC50 = 2300.0 nM 5.64
CHEMBL1782533 IC50 = 2400.0 nM 5.62
CHEMBL1782529 IC50 = 2700.0 nM 5.57
CHEMBL1782523 IC50 = 4500.0 nM 5.35
CHEMBL1782519 IC50 = 4900.0 nM 5.31
CHEMBL1782505 IC50 = 5300.0 nM 5.28
CHEMBL1782508 IC50 = 5400.0 nM 5.27
CHEMBL1738915 IC50 = 5800.0 nM 5.24
CHEMBL1782510 IC50 = 6000.0 nM 5.22
CHEMBL1782506 IC50 = 6100.0 nM 5.21
CHEMBL1782507 IC50 = 7400.0 nM 5.13
CHEMBL1204914 IC50 = 7800.0 nM 5.11
CHEMBL1738916 IC50 = 8500.0 nM 5.07
CHEMBL84095 IC50 = 119000.0 nM -