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Assay Detail

CHEMBL887076

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

Binding
Inhibition of Tie2 after 90 mins by HTRF assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Angiopoietin-1 receptor (CHEMBL4128)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Caenepeel S, Cee VJ, Chaffee SC, Emery M, Fretland J, Gallant P, Gu Y, Johnson RE, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Wang L, Zhao H.
Bioorg Med Chem Lett (2007) 17 : 2886 -2889
PubMed 17350837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.27 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL245744 1 9.00
CHEMBL245746 1 9.00
CHEMBL245947 1 9.00
CHEMBL221484 1 9.00
CHEMBL394693 1 8.70
CHEMBL245745 1 8.52
CHEMBL246150 1 8.40
CHEMBL394694 1 8.40
CHEMBL245948 1 8.22
CHEMBL246151 1 8.22
CHEMBL246152 1 8.10
CHEMBL397090 1 8.05
CHEMBL394692 1 7.89
CHEMBL246356 1 7.80
CHEMBL246355 1 7.77
CHEMBL245549 1 7.77
CHEMBL397089 1 7.70
CHEMBL245949 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL245744 IC50 = 1.0 nM 9.00
CHEMBL245746 IC50 = 1.0 nM 9.00
CHEMBL245947 IC50 = 1.0 nM 9.00
CHEMBL221484 IC50 = 1.0 nM 9.00
CHEMBL394693 IC50 = 2.0 nM 8.70
CHEMBL245745 IC50 = 3.0 nM 8.52
CHEMBL246150 IC50 = 4.0 nM 8.40
CHEMBL394694 IC50 = 4.0 nM 8.40
CHEMBL245948 IC50 = 6.0 nM 8.22
CHEMBL246151 IC50 = 6.0 nM 8.22
CHEMBL246152 IC50 = 8.0 nM 8.10
CHEMBL397090 IC50 = 9.0 nM 8.05
CHEMBL394692 IC50 = 13.0 nM 7.89
CHEMBL246356 IC50 = 16.0 nM 7.80
CHEMBL246355 IC50 = 17.0 nM 7.77
CHEMBL245549 IC50 = 17.0 nM 7.77
CHEMBL397089 IC50 = 20.0 nM 7.70
CHEMBL245949 IC50 = 55.0 nM 7.26