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Assay Detail

CHEMBL4407299

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

Binding
Binding affinity to Mycobacterium abscessus N-terminal His-tagged 3C protease linked full length tRNA (m1-G37) methyltransferase expressed in Escherichia coli BL21(DE3) by isothermal titration calorimetry
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacteroides abscessus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Development of Inhibitors against <i>Mycobacterium abscessus</i> tRNA (m<sup>1</sup>G37) Methyltransferase (TrmD) Using Fragment-Based Approaches.
Whitehouse AJ, Thomas SE, Brown KP, Fanourakis A, Chan DS, Libardo MDJ, Mendes V, Boshoff HIM, Floto RA, Abell C, Blundell TL, Coyne AG.
J Med Chem (2019) 62 : 7210 -7232
PubMed 31282680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 49 4.96 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4576907 1 6.92
CHEMBL4583591 1 6.75
CHEMBL4585013 1 6.44
CHEMBL4454013 1 6.30
CHEMBL4551843 1 6.23
CHEMBL4435815 1 5.89
CHEMBL4471268 1 5.50
CHEMBL4519568 1 5.34
CHEMBL4548872 1 5.30
CHEMBL4447182 1 5.17
CHEMBL4434680 1 5.07
CHEMBL4541236 1 5.00
CHEMBL4517357 1 5.00
CHEMBL4446084 1 4.96
CHEMBL4572807 1 4.92
CHEMBL4531919 1 4.92
CHEMBL4461645 1 4.92
CHEMBL4571359 1 4.89
CHEMBL4583556 1 4.85
CHEMBL4537315 1 4.72
CHEMBL4537643 1 4.57
CHEMBL4526104 1 4.52
CHEMBL4536428 1 4.48
CHEMBL4474548 1 4.23
CHEMBL4453792 1 4.16
CHEMBL4457380 1 4.14
CHEMBL4461273 1 4.05
CHEMBL4449229 1 4.04
CHEMBL4567409 1 4.00
CHEMBL4475938 1 3.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4576907 Kd = 120.0 nM 6.92
CHEMBL4583591 Kd = 180.0 nM 6.75
CHEMBL4585013 Kd = 360.0 nM 6.44
CHEMBL4454013 Kd = 500.0 nM 6.30
CHEMBL4551843 Kd = 590.0 nM 6.23
CHEMBL4435815 Kd = 1300.0 nM 5.89
CHEMBL4471268 Kd = 3200.0 nM 5.50
CHEMBL4519568 Kd = 4600.0 nM 5.34
CHEMBL4548872 Kd = 5000.0 nM 5.30
CHEMBL4447182 Kd = 6700.0 nM 5.17
CHEMBL4434680 Kd = 8500.0 nM 5.07
CHEMBL4541236 Kd = 10000.0 nM 5.00
CHEMBL4517357 Kd = 10000.0 nM 5.00
CHEMBL4446084 Kd = 11000.0 nM 4.96
CHEMBL4461645 Kd = 12000.0 nM 4.92
CHEMBL4572807 Kd = 12000.0 nM 4.92
CHEMBL4531919 Kd = 12000.0 nM 4.92
CHEMBL4571359 Kd = 13000.0 nM 4.89
CHEMBL4583556 Kd = 14000.0 nM 4.85
CHEMBL4537315 Kd = 19000.0 nM 4.72
CHEMBL4537643 Kd = 27000.0 nM 4.57
CHEMBL4526104 Kd = 30000.0 nM 4.52
CHEMBL4536428 Kd = 33000.0 nM 4.48
CHEMBL4474548 Kd = 59000.0 nM 4.23
CHEMBL4453792 Kd = 70000.0 nM 4.16
CHEMBL4457380 Kd = 73000.0 nM 4.14
CHEMBL4461273 Kd = 89000.0 nM 4.05
CHEMBL4449229 Kd = 92000.0 nM 4.04
CHEMBL4567409 Kd = 100000.0 nM 4.00
CHEMBL4475938 Kd = 110000.0 nM 3.96
CHEMBL3751985 Kd = 170000.0 nM 3.77
CHEMBL4071778 Kd = 260000.0 nM 3.58
CHEMBL4532147 Kd - -
CHEMBL4525649 Kd - -
CHEMBL4440886 Kd - -
CHEMBL4533375 Kd - -
CHEMBL4446155 Kd - -
CHEMBL1650269 Kd - -
CHEMBL1483289 Kd - -
CHEMBL4454136 Kd - -
CHEMBL1229732 Kd - -
CHEMBL342460 Kd - -
CHEMBL4550520 Kd - -
CHEMBL4534988 Kd - -
CHEMBL4564248 Kd - -
CHEMBL4536748 Kd = 490000.0 nM -
CHEMBL4466923 Kd = 2000000.0 nM -
CHEMBL4434796 Kd = 190000.0 nM -
CHEMBL4459768 Kd = 710000.0 nM -