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Assay Detail

CHEMBL917014

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

Binding
Inhibition of human uPA
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 Intermediate

Target

Urokinase-type plasminogen activator (CHEMBL3286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines.
Fish PV, Barber CG, Brown DG, Butt R, Collis MG, Dickinson RP, Henry BT, Horne VA, Huggins JP, King E, O'Gara M, McCleverty D, McIntosh F, Phillips C, Webster R.
J Med Chem (2007) 50 : 2341 -2351
PubMed 17447747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 7.50 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226714 1 8.85
CHEMBL228113 1 8.80
CHEMBL227607 1 8.59
CHEMBL374378 1 8.24
CHEMBL227666 1 8.13
CHEMBL228170 1 8.13
CHEMBL227976 1 8.10
CHEMBL227421 1 8.00
CHEMBL227990 1 8.00
CHEMBL227931 1 8.00
CHEMBL228204 1 7.96
CHEMBL227890 1 7.96
CHEMBL228173 1 7.85
CHEMBL227422 1 7.72
CHEMBL223864 1 7.68
CHEMBL266435 1 7.66
CHEMBL388780 1 7.64
CHEMBL376763 1 7.57
CHEMBL227426 1 7.55
CHEMBL228172 1 7.54
CHEMBL427456 1 7.52
CHEMBL227425 1 7.51
CHEMBL227995 1 7.46
CHEMBL227606 1 7.37
CHEMBL226716 1 7.32
CHEMBL390133 1 7.27
CHEMBL227664 1 7.27
CHEMBL227584 1 7.24
CHEMBL224689 1 7.23
CHEMBL389056 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226714 Ki = 1.4 nM 8.85
CHEMBL228113 Ki = 1.6 nM 8.80
CHEMBL227607 Ki = 2.6 nM 8.59
CHEMBL374378 Ki = 5.8 nM 8.24
CHEMBL227666 Ki = 7.4 nM 8.13
CHEMBL228170 Ki = 7.4 nM 8.13
CHEMBL227976 Ki = 8.0 nM 8.10
CHEMBL227421 Ki = 10.0 nM 8.00
CHEMBL227990 Ki = 9.9 nM 8.00
CHEMBL227931 Ki = 10.0 nM 8.00
CHEMBL228204 Ki = 11.0 nM 7.96
CHEMBL227890 Ki = 11.0 nM 7.96
CHEMBL228173 Ki = 14.0 nM 7.85
CHEMBL227422 Ki = 19.0 nM 7.72
CHEMBL223864 Ki = 21.0 nM 7.68
CHEMBL266435 Ki = 22.0 nM 7.66
CHEMBL388780 Ki = 23.0 nM 7.64
CHEMBL376763 Ki = 27.0 nM 7.57
CHEMBL227426 Ki = 28.0 nM 7.55
CHEMBL228172 Ki = 29.0 nM 7.54
CHEMBL427456 Ki = 30.0 nM 7.52
CHEMBL227425 Ki = 31.0 nM 7.51
CHEMBL227995 Ki = 35.0 nM 7.46
CHEMBL227606 Ki = 43.0 nM 7.37
CHEMBL226716 Ki = 48.0 nM 7.32
CHEMBL390133 Ki = 54.0 nM 7.27
CHEMBL227664 Ki = 54.0 nM 7.27
CHEMBL227584 Ki = 58.0 nM 7.24
CHEMBL224689 Ki = 59.0 nM 7.23
CHEMBL389056 Ki = 66.0 nM 7.18
CHEMBL228052 Ki = 67.0 nM 7.17
CHEMBL390310 Ki = 71.0 nM 7.15
CHEMBL374623 Ki = 86.0 nM 7.07
CHEMBL228238 Ki = 111.0 nM 6.96
CHEMBL227940 Ki = 130.0 nM 6.89
CHEMBL227782 Ki = 140.0 nM 6.85
CHEMBL389032 Ki = 160.0 nM 6.80
CHEMBL227781 Ki = 160.0 nM 6.80
CHEMBL227583 Ki = 280.0 nM 6.55
CHEMBL227769 Ki = 330.0 nM 6.48
CHEMBL228051 Ki = 330.0 nM 6.48
CHEMBL227770 Ki = 550.0 nM 6.26