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Assay Detail

CHEMBL894022

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

Binding
Inhibition of human recombinant MetAP2
ChEMBL ↗
94
Total Activities
94
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

Methionine aminopeptidase 2 (CHEMBL3922) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
Marino JP, Fisher PW, Hofmann GA, Kirkpatrick RB, Janson CA, Johnson RK, Ma C, Mattern M, Meek TD, Ryan MD, Schulz C, Smith WW, Tew DG, Tomazek TA, Veber DF, Xiong WC, Yamamoto Y, Yamashita K, Yang G, Thompson SK.
J Med Chem (2007) 50 : 3777 -3785
PubMed 17636946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 94 8.42 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243306 — — 1 10.40
CHEMBL241829 — — 1 10.40
CHEMBL397477 — — 1 10.30
CHEMBL243111 — — 1 10.15
CHEMBL242435 — — 1 9.89
CHEMBL245022 — — 1 9.82
CHEMBL245226 — — 1 9.80
CHEMBL389087 — — 1 9.64
CHEMBL242050 — — 1 9.52
CHEMBL242875 — — 1 9.39
CHEMBL242028 — — 1 9.37
CHEMBL243303 — — 1 9.30
CHEMBL243101 — — 1 9.30
CHEMBL242051 — — 1 9.30
CHEMBL242891 — — 1 9.28
CHEMBL242462 — — 1 9.21
CHEMBL243320 — — 1 9.19
CHEMBL242663 — — 1 9.15
CHEMBL243305 — — 1 9.12
CHEMBL396988 — — 1 9.10
CHEMBL242447 — — 1 9.05
CHEMBL242876 — — 1 9.05
CHEMBL430001 — — 1 9.05
CHEMBL230640 — — 1 9.00
CHEMBL424278 O-CHLOROACETYLCARBAMOYLFUMAGILLOL 2.0 1 9.00
CHEMBL398002 — — 1 8.92
CHEMBL396742 — — 1 8.89
CHEMBL243746 — — 1 8.89
CHEMBL242464 — — 1 8.82
CHEMBL395100 — — 1 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243306 — Ki = 0.04 nM 10.40
CHEMBL241829 — Ki = 0.04 nM 10.40
CHEMBL397477 — Ki = 0.05 nM 10.30
CHEMBL243111 — Ki = 0.07 nM 10.15
CHEMBL242435 — Ki = 0.13 nM 9.89
CHEMBL245022 — Ki = 0.15 nM 9.82
CHEMBL245226 — Ki = 0.16 nM 9.80
CHEMBL389087 — Ki = 0.23 nM 9.64
CHEMBL242050 — Ki = 0.3 nM 9.52
CHEMBL242875 — Ki = 0.41 nM 9.39
CHEMBL242028 — Ki = 0.43 nM 9.37
CHEMBL243303 — Ki = 0.5 nM 9.30
CHEMBL243101 — Ki = 0.5 nM 9.30
CHEMBL242051 — Ki = 0.5 nM 9.30
CHEMBL242891 — Ki = 0.52 nM 9.28
CHEMBL242462 — Ki = 0.61 nM 9.21
CHEMBL243320 — Ki = 0.65 nM 9.19
CHEMBL242663 — Ki = 0.7 nM 9.15
CHEMBL243305 — Ki = 0.75 nM 9.12
CHEMBL396988 — Ki = 0.8 nM 9.10
CHEMBL242447 — Ki = 0.9 nM 9.05
CHEMBL242876 — Ki = 0.9 nM 9.05
CHEMBL430001 — Ki = 0.9 nM 9.05
CHEMBL230640 — Ki = 1.0 nM 9.00
CHEMBL424278 O-CHLOROACETYLCARBAMOYLFUMAGILLOL Ki = 1.0 nM 9.00
CHEMBL398002 — Ki = 1.2 nM 8.92
CHEMBL243746 — Ki = 1.3 nM 8.89
CHEMBL396742 — Ki = 1.3 nM 8.89
CHEMBL242464 — Ki = 1.5 nM 8.82
CHEMBL395100 — Ki = 1.5 nM 8.82
CHEMBL245227 — Ki = 1.6 nM 8.80
CHEMBL242049 — Ki = 1.7 nM 8.77
CHEMBL245228 — Ki = 1.7 nM 8.77
CHEMBL243117 — Ki = 1.8 nM 8.74
CHEMBL230641 — Ki = 2.0 nM 8.70
CHEMBL242646 — Ki = 2.1 nM 8.68
CHEMBL397244 — Ki = 2.4 nM 8.62
CHEMBL396468 — Ki = 2.5 nM 8.60
CHEMBL242678 — Ki = 2.5 nM 8.60
CHEMBL243100 — Ki = 2.7 nM 8.57
CHEMBL242272 — Ki = 3.0 nM 8.52
CHEMBL444369 — Ki = 3.0 nM 8.52
CHEMBL245007 — Ki = 3.1 nM 8.51
CHEMBL243321 — Ki = 3.3 nM 8.48
CHEMBL245021 — Ki = 3.3 nM 8.48
CHEMBL242461 — Ki = 3.5 nM 8.46
CHEMBL243110 — Ki = 3.6 nM 8.44
CHEMBL398228 — Ki = 3.7 nM 8.43
CHEMBL395481 — Ki = 3.8 nM 8.42
CHEMBL243102 — Ki = 3.8 nM 8.42