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Assay Detail

CHEMBL815983

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Binding
In vitro inhibitory activity against Urokinase-type plasminogen activator (microPa)
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors.
Wilson KJ, Illig CR, Subasinghe N, Hoffman JB, Rudolph MJ, Soll R, Molloy CJ, Bone R, Green D, Randall T, Zhang M, Lewandowski FA, Zhou Z, Sharp C, Maguire D, Grasberger B, DesJarlais RL, Spurlino J.
Bioorg Med Chem Lett (2001) 11 : 915 -918
PubMed 11294390 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 6.33 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL173681 — — 1 7.22
CHEMBL173906 — — 1 7.16
CHEMBL352562 — — 1 7.10
CHEMBL353872 — — 1 6.96
CHEMBL173981 — — 1 6.96
CHEMBL353478 — — 1 6.80
CHEMBL172637 — — 1 6.77
CHEMBL172934 — — 1 6.75
CHEMBL171353 — — 1 6.75
CHEMBL355341 — — 1 6.75
CHEMBL171245 — — 1 6.70
CHEMBL441839 — — 1 6.62
CHEMBL369810 — — 1 6.55
CHEMBL355095 — — 1 6.55
CHEMBL172162 — — 1 6.55
CHEMBL171469 — — 1 6.55
CHEMBL173096 — — 1 6.55
CHEMBL173211 — — 1 6.51
CHEMBL60088 — — 1 6.50
CHEMBL355531 — — 1 6.46
CHEMBL171715 — — 1 6.40
CHEMBL171642 — — 1 6.37
CHEMBL353655 — — 1 6.36
CHEMBL171514 — — 1 6.32
CHEMBL170410 — — 1 6.30
CHEMBL367114 — — 1 6.28
CHEMBL173392 — — 1 6.19
CHEMBL173065 — — 1 6.18
CHEMBL172982 — — 1 6.16
CHEMBL174193 — — 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL173681 — Ki = 60.0 nM 7.22
CHEMBL173906 — Ki = 70.0 nM 7.16
CHEMBL352562 — Ki = 80.0 nM 7.10
CHEMBL353872 — Ki = 110.0 nM 6.96
CHEMBL173981 — Ki = 110.0 nM 6.96
CHEMBL353478 — Ki = 160.0 nM 6.80
CHEMBL172637 — Ki = 170.0 nM 6.77
CHEMBL172934 — Ki = 180.0 nM 6.75
CHEMBL171353 — Ki = 180.0 nM 6.75
CHEMBL355341 — Ki = 180.0 nM 6.75
CHEMBL171245 — Ki = 200.0 nM 6.70
CHEMBL441839 — Ki = 240.0 nM 6.62
CHEMBL173096 — Ki = 280.0 nM 6.55
CHEMBL355095 — Ki = 280.0 nM 6.55
CHEMBL369810 — Ki = 280.0 nM 6.55
CHEMBL172162 — Ki = 280.0 nM 6.55
CHEMBL171469 — Ki = 280.0 nM 6.55
CHEMBL173211 — Ki = 310.0 nM 6.51
CHEMBL60088 — Ki = 320.0 nM 6.50
CHEMBL355531 — Ki = 350.0 nM 6.46
CHEMBL171715 — Ki = 400.0 nM 6.40
CHEMBL171642 — Ki = 430.0 nM 6.37
CHEMBL353655 — Ki = 440.0 nM 6.36
CHEMBL171514 — Ki = 480.0 nM 6.32
CHEMBL170410 — Ki = 500.0 nM 6.30
CHEMBL367114 — Ki = 520.0 nM 6.28
CHEMBL173392 — Ki = 640.0 nM 6.19
CHEMBL173065 — Ki = 660.0 nM 6.18
CHEMBL172982 — Ki = 700.0 nM 6.16
CHEMBL174193 — Ki = 910.0 nM 6.04
CHEMBL170363 — Ki = 1020.0 nM 5.99
CHEMBL440932 — Ki = 1100.0 nM 5.96
CHEMBL352875 — Ki = 1110.0 nM 5.96
CHEMBL170477 — Ki = 1180.0 nM 5.93
CHEMBL172150 — Ki = 1400.0 nM 5.85
CHEMBL353665 — Ki = 1460.0 nM 5.84
CHEMBL354109 — Ki = 1500.0 nM 5.82
CHEMBL173483 — Ki = 1600.0 nM 5.80
CHEMBL369272 — Ki = 1620.0 nM 5.79
CHEMBL171270 — Ki = 1840.0 nM 5.74
CHEMBL355618 — Ki = 3060.0 nM 5.51
CHEMBL172671 — Ki = 3900.0 nM 5.41
CHEMBL173953 — Ki = 6000.0 nM 5.22