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Assay Detail

CHEMBL1942547

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Binding
Activation of human PKM2 assessed as ATP product formation after 1 hr by luminescent pyruvate kinase-luciferase coupled assay
ChEMBL ↗
81
Total Activities
81
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Pyruvate kinase PKM (CHEMBL1075189) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M, Auld DS, Thomas CJ, Boxer MB.
Bioorg Med Chem Lett (2011) 21 : 6322 -6327
PubMed 21958545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 77 5.92 7.42
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1089334 — — 1 7.42
CHEMBL1939112 — — 1 7.22
CHEMBL1939115 — — 1 7.16
CHEMBL1085587 — — 1 7.14
CHEMBL1939110 — — 1 7.05
CHEMBL1939116 — — 1 7.05
CHEMBL1939085 — — 1 7.00
CHEMBL1939113 — — 1 6.89
CHEMBL1939108 — — 1 6.85
CHEMBL1939107 — — 1 6.77
CHEMBL1939104 — — 1 6.75
CHEMBL1939117 — — 1 6.68
CHEMBL1939095 — — 1 6.68
CHEMBL1939096 — — 1 6.66
CHEMBL1939105 — — 1 6.64
CHEMBL1939111 — — 1 6.62
CHEMBL1311880 — — 1 6.60
CHEMBL1939094 — — 1 6.58
CHEMBL1939089 — — 1 6.54
CHEMBL1939114 — — 1 6.54
CHEMBL1877309 — — 1 6.39
CHEMBL1939090 — — 1 6.36
CHEMBL1939098 — — 1 6.36
CHEMBL1939093 — — 1 6.32
CHEMBL1939099 — — 1 6.29
CHEMBL1939088 — — 1 6.27
CHEMBL1939087 — — 1 6.25
CHEMBL1939102 — — 1 6.24
CHEMBL1939109 — — 1 6.22
CHEMBL1509101 — — 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1089334 — EC50 = 38.0 nM 7.42
CHEMBL1939112 — EC50 = 60.0 nM 7.22
CHEMBL1939115 — EC50 = 70.0 nM 7.16
CHEMBL1085587 — EC50 = 73.0 nM 7.14
CHEMBL1939110 — EC50 = 90.0 nM 7.05
CHEMBL1939116 — EC50 = 90.0 nM 7.05
CHEMBL1939085 — EC50 = 100.0 nM 7.00
CHEMBL1939113 — EC50 = 130.0 nM 6.89
CHEMBL1939108 — EC50 = 140.0 nM 6.85
CHEMBL1939107 — EC50 = 170.0 nM 6.77
CHEMBL1939104 — EC50 = 180.0 nM 6.75
CHEMBL1939117 — EC50 = 210.0 nM 6.68
CHEMBL1939095 — EC50 = 210.0 nM 6.68
CHEMBL1939096 — EC50 = 220.0 nM 6.66
CHEMBL1939105 — EC50 = 230.0 nM 6.64
CHEMBL1939111 — EC50 = 240.0 nM 6.62
CHEMBL1311880 — EC50 = 250.0 nM 6.60
CHEMBL1939094 — EC50 = 260.0 nM 6.58
CHEMBL1939089 — EC50 = 290.0 nM 6.54
CHEMBL1939114 — EC50 = 290.0 nM 6.54
CHEMBL1877309 — EC50 = 410.0 nM 6.39
CHEMBL1939090 — EC50 = 440.0 nM 6.36
CHEMBL1939098 — EC50 = 440.0 nM 6.36
CHEMBL1939093 — EC50 = 480.0 nM 6.32
CHEMBL1939099 — EC50 = 510.0 nM 6.29
CHEMBL1939088 — EC50 = 540.0 nM 6.27
CHEMBL1939087 — EC50 = 560.0 nM 6.25
CHEMBL1939102 — EC50 = 570.0 nM 6.24
CHEMBL1939109 — EC50 = 600.0 nM 6.22
CHEMBL1509101 — EC50 = 790.0 nM 6.10
CHEMBL1938918 — EC50 = 790.0 nM 6.10
CHEMBL1939106 — EC50 = 880.0 nM 6.06
CHEMBL1938914 — EC50 = 940.0 nM 6.03
CHEMBL1939078 — EC50 = 1100.0 nM 5.96
CHEMBL1939082 — EC50 = 1300.0 nM 5.89
CHEMBL1939086 — EC50 = 1300.0 nM 5.89
CHEMBL1413238 — EC50 = 1400.0 nM 5.85
CHEMBL1938916 — EC50 = 1500.0 nM 5.82
CHEMBL1939074 — EC50 = 2000.0 nM 5.70
CHEMBL1939103 — EC50 = 2100.0 nM 5.68
CHEMBL1938917 — EC50 = 2200.0 nM 5.66
CHEMBL1938915 — EC50 = 2300.0 nM 5.64
CHEMBL1939097 — EC50 = 3800.0 nM 5.42
CHEMBL1377752 — EC50 = 4300.0 nM 5.37
CHEMBL1939084 — EC50 = 4600.0 nM 5.34
CHEMBL1514868 — EC50 = 5200.0 nM 5.28
CHEMBL1938913 — EC50 = 6000.0 nM 5.22
CHEMBL1358228 — EC50 = 6000.0 nM 5.22
CHEMBL1939120 — EC50 = 6100.0 nM 5.21
CHEMBL1939121 — EC50 = 6100.0 nM 5.21