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Assay Detail

CHEMBL1109141

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

Binding
Inhibition of GST-tagged PLK1 expressed in H5 insect cells assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase PLK1 (CHEMBL3024) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors.
Beria I, Ballinari D, Bertrand JA, Borghi D, Bossi RT, Brasca MG, Cappella P, Caruso M, Ceccarelli W, Ciavolella A, Cristiani C, Croci V, De Ponti A, Fachin G, Ferguson RD, Lansen J, Moll JK, Pesenti E, Posteri H, Perego R, Rocchetti M, Storici P, Volpi D, Valsasina B.
J Med Chem (2010) 53 : 3532 -3551
PubMed 20397705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.57 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1095709 — — 1 8.22
CHEMBL1094408 NMS-1286937 — 1 8.15
CHEMBL1094477 — — 1 7.82
CHEMBL1095717 — — 1 7.40
CHEMBL1094135 — — 1 7.38
CHEMBL1097424 — — 1 7.29
CHEMBL559845 — — 1 7.17
CHEMBL1094478 — — 1 7.01
CHEMBL1099105 — — 1 7.00
CHEMBL1095457 — — 1 6.96
CHEMBL1098060 — — 1 6.96
CHEMBL1095716 — — 1 6.96
CHEMBL1095771 — — 1 6.90
CHEMBL1095448 — — 1 6.87
CHEMBL1094402 — — 1 6.84
CHEMBL1097022 — — 1 6.82
CHEMBL1099106 — — 1 6.71
CHEMBL1094401 — — 1 6.61
CHEMBL1094322 — — 1 6.59
CHEMBL1096095 — — 1 6.56
CHEMBL1099104 — — 1 6.46
CHEMBL1095772 — — 1 6.44
CHEMBL1097071 — — 1 6.37
CHEMBL1094735 — — 1 6.37
CHEMBL1096028 — — 1 6.33
CHEMBL1094810 — — 1 6.31
CHEMBL1097429 — — 1 6.06
CHEMBL1094488 — — 1 6.03
CHEMBL1094820 — — 1 6.02
CHEMBL1094484 — — 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1095709 — IC50 = 6.0 nM 8.22
CHEMBL1094408 NMS-1286937 IC50 = 7.0 nM 8.15
CHEMBL1094477 — IC50 = 15.0 nM 7.82
CHEMBL1095717 — IC50 = 40.0 nM 7.40
CHEMBL1094135 — IC50 = 42.0 nM 7.38
CHEMBL1097424 — IC50 = 51.0 nM 7.29
CHEMBL559845 — IC50 = 68.0 nM 7.17
CHEMBL1094478 — IC50 = 97.0 nM 7.01
CHEMBL1099105 — IC50 = 100.0 nM 7.00
CHEMBL1095457 — IC50 = 110.0 nM 6.96
CHEMBL1098060 — IC50 = 110.0 nM 6.96
CHEMBL1095716 — IC50 = 109.0 nM 6.96
CHEMBL1095771 — IC50 = 125.0 nM 6.90
CHEMBL1095448 — IC50 = 135.0 nM 6.87
CHEMBL1094402 — IC50 = 143.0 nM 6.84
CHEMBL1097022 — IC50 = 150.0 nM 6.82
CHEMBL1099106 — IC50 = 197.0 nM 6.71
CHEMBL1094401 — IC50 = 248.0 nM 6.61
CHEMBL1094322 — IC50 = 256.0 nM 6.59
CHEMBL1096095 — IC50 = 278.0 nM 6.56
CHEMBL1099104 — IC50 = 346.0 nM 6.46
CHEMBL1095772 — IC50 = 365.0 nM 6.44
CHEMBL1094735 — IC50 = 430.0 nM 6.37
CHEMBL1097071 — IC50 = 432.0 nM 6.37
CHEMBL1096028 — IC50 = 464.0 nM 6.33
CHEMBL1094810 — IC50 = 488.0 nM 6.31
CHEMBL1097429 — IC50 = 872.0 nM 6.06
CHEMBL1094488 — IC50 = 943.0 nM 6.03
CHEMBL1094820 — IC50 = 949.0 nM 6.02
CHEMBL1094484 — IC50 = 1117.0 nM 5.95
CHEMBL1094817 — IC50 = 1565.0 nM 5.80
CHEMBL1094821 — IC50 = 1969.0 nM 5.71
CHEMBL1094822 — IC50 = 2033.0 nM 5.69
CHEMBL1097374 — IC50 = 2051.0 nM 5.69
CHEMBL1094815 — IC50 = 2076.0 nM 5.68
CHEMBL1097373 — IC50 = 2523.0 nM 5.60
CHEMBL1094816 — IC50 = 3733.0 nM 5.43
CHEMBL562104 — IC50 = 4215.0 nM 5.38
CHEMBL1098059 — IC50 > 10000.0 nM -
CHEMBL559639 — IC50 > 10000.0 nM -
CHEMBL563028 — IC50 > 10000.0 nM -
CHEMBL1098058 — IC50 > 10000.0 nM -
CHEMBL563150 — IC50 > 10000.0 nM -
CHEMBL1094400 — IC50 > 10000.0 nM -
CHEMBL1098057 — IC50 > 10000.0 nM -
CHEMBL1095132 — IC50 > 10000.0 nM -
CHEMBL1094811 — IC50 > 10000.0 nM -