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Assay Detail

CHEMBL3734233

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

Binding
Inhibition of N-terminally GST-tagged human DLK catalytic domain (1 to 520 amino acids) using N- terminal His-tagged MKK4 K131M substrate incubated for 60 mins by TR-FRET assay
ChEMBL ↗
503
Total Activities
427
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase kinase kinase 12 (CHEMBL1908389) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Biheteroaryl compounds and uses thereof
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 503 7.70 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3733088 — — 2 10.22
CHEMBL3729613 — — 1 9.51
CHEMBL3732543 — — 2 9.40
CHEMBL3730823 — — 1 9.29
CHEMBL3731122 — — 1 9.28
CHEMBL3732528 — — 2 9.25
CHEMBL3728902 — — 1 9.24
CHEMBL3733275 — — 1 9.11
CHEMBL3728441 — — 2 9.05
CHEMBL3732975 — — 2 9.04
CHEMBL3732447 — — 1 9.04
CHEMBL3732912 — — 1 9.00
CHEMBL3727796 — — 1 9.00
CHEMBL3732012 GDC-0134 1.0 1 9.00
CHEMBL3730912 — — 1 9.00
CHEMBL3727449 — — 1 9.00
CHEMBL3729148 — — 1 9.00
CHEMBL3727397 — — 1 9.00
CHEMBL3732360 — — 1 9.00
CHEMBL3730273 — — 1 9.00
CHEMBL3731284 — — 1 9.00
CHEMBL3728651 — — 2 8.96
CHEMBL3731609 — — 1 8.94
CHEMBL3728354 — — 2 8.93
CHEMBL3729696 — — 1 8.92
CHEMBL3732684 — — 1 8.90
CHEMBL3730558 — — 2 8.85
CHEMBL3727385 — — 1 8.83
CHEMBL3731242 — — 2 8.78
CHEMBL3731498 — — 1 8.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3733088 — Ki = 0.06 nM 10.22
CHEMBL3729613 — Ki = 0.31 nM 9.51
CHEMBL3732543 — Ki = 0.4 nM 9.40
CHEMBL3730823 — Ki = 0.51 nM 9.29
CHEMBL3731122 — Ki = 0.52 nM 9.28
CHEMBL3732528 — Ki = 0.56 nM 9.25
CHEMBL3728902 — Ki = 0.574 nM 9.24
CHEMBL3733275 — Ki = 0.77 nM 9.11
CHEMBL3728441 — Ki = 0.9 nM 9.05
CHEMBL3732447 — Ki = 0.92 nM 9.04
CHEMBL3732975 — Ki = 0.91 nM 9.04
CHEMBL3732912 — Ki = 1.0 nM 9.00
CHEMBL3727449 — Ki = 1.0 nM 9.00
CHEMBL3730273 — Ki = 1.0 nM 9.00
CHEMBL3732360 — Ki = 1.0 nM 9.00
CHEMBL3730912 — Ki = 1.0 nM 9.00
CHEMBL3727796 — Ki = 1.0 nM 9.00
CHEMBL3731284 — Ki = 1.0 nM 9.00
CHEMBL3727397 — Ki = 1.0 nM 9.00
CHEMBL3732012 GDC-0134 Ki = 1.0 nM 9.00
CHEMBL3729148 — Ki = 1.0 nM 9.00
CHEMBL3728651 — Ki = 1.09 nM 8.96
CHEMBL3731609 — Ki = 1.14 nM 8.94
CHEMBL3728354 — Ki = 1.17 nM 8.93
CHEMBL3729696 — Ki = 1.2 nM 8.92
CHEMBL3732684 — Ki = 1.25 nM 8.90
CHEMBL3730558 — Ki = 1.41 nM 8.85
CHEMBL3727385 — Ki = 1.47 nM 8.83
CHEMBL3731242 — Ki = 1.65 nM 8.78
CHEMBL3731498 — Ki = 1.76 nM 8.75
CHEMBL3733255 — Ki = 1.85 nM 8.73
CHEMBL3729681 — Ki = 1.92 nM 8.72
CHEMBL3728682 — Ki = 1.93 nM 8.71
CHEMBL3728287 — Ki = 1.93 nM 8.71
CHEMBL3729369 — Ki = 2.0 nM 8.70
CHEMBL3729389 — Ki = 2.02 nM 8.70
CHEMBL3728219 — Ki = 2.0 nM 8.70
CHEMBL3731156 — Ki = 2.0 nM 8.70
CHEMBL3727991 — Ki = 2.0 nM 8.70
CHEMBL3729085 — Ki = 1.99 nM 8.70
CHEMBL3731916 — Ki = 2.06 nM 8.69
CHEMBL3731405 — Ki = 2.3 nM 8.64
CHEMBL3733363 — Ki = 2.27 nM 8.64
CHEMBL3732989 — Ki = 2.3 nM 8.64
CHEMBL3732975 — Ki = 2.35 nM 8.63
CHEMBL3732685 — Ki = 2.35 nM 8.63
CHEMBL3732366 — Ki = 2.59 nM 8.59
CHEMBL3732536 — Ki = 2.62 nM 8.58
CHEMBL3730695 — Ki = 2.62 nM 8.58
CHEMBL3731453 — Ki = 2.67 nM 8.57