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Assay Detail

CHEMBL4392494

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Binding
Inhibition of human ERG
49
Total Activities
49
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

Publication

Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP.
Bioorg Med Chem Lett (2019) 29 : 1380 -1385
PubMed 30952592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 49 5.24 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4447657 1 6.37
CHEMBL4472207 1 6.21
CHEMBL4453601 1 6.09
CHEMBL4467163 1 5.87
CHEMBL4525823 1 5.85
CHEMBL4575608 1 5.79
CHEMBL4562424 1 5.76
CHEMBL4516271 1 5.70
CHEMBL4443018 1 5.65
CHEMBL4541477 1 5.64
CHEMBL4561313 1 5.57
CHEMBL4452750 1 5.52
CHEMBL4453443 1 5.52
CHEMBL4554202 1 5.45
CHEMBL2408633 1 5.45
CHEMBL4461413 1 5.43
CHEMBL4458847 1 5.42
CHEMBL4464262 1 5.39
CHEMBL4452940 1 5.39
CHEMBL4473500 1 5.35
CHEMBL4476596 1 5.32
CHEMBL4572398 1 5.31
CHEMBL4450287 1 5.28
CHEMBL2408632 1 5.27
CHEMBL4527223 1 5.18
CHEMBL4483357 1 5.09
CHEMBL4585408 1 5.09
CHEMBL4592144 1 5.07
CHEMBL4461148 1 4.97
CHEMBL4461166 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4447657 Ki = 426.0 nM 6.37
CHEMBL4472207 Ki = 616.0 nM 6.21
CHEMBL4453601 Ki = 820.0 nM 6.09
CHEMBL4467163 Ki = 1360.0 nM 5.87
CHEMBL4525823 Ki = 1427.0 nM 5.85
CHEMBL4575608 Ki = 1641.0 nM 5.79
CHEMBL4562424 Ki = 1740.0 nM 5.76
CHEMBL4516271 Ki = 1980.0 nM 5.70
CHEMBL4443018 Ki = 2250.0 nM 5.65
CHEMBL4541477 Ki = 2314.0 nM 5.64
CHEMBL4561313 Ki = 2700.0 nM 5.57
CHEMBL4452750 Ki = 3000.0 nM 5.52
CHEMBL4453443 Ki = 3000.0 nM 5.52
CHEMBL4554202 Ki = 3560.0 nM 5.45
CHEMBL2408633 Ki = 3520.0 nM 5.45
CHEMBL4461413 Ki = 3750.0 nM 5.43
CHEMBL4458847 Ki = 3800.0 nM 5.42
CHEMBL4464262 Ki = 4100.0 nM 5.39
CHEMBL4452940 Ki = 4100.0 nM 5.39
CHEMBL4473500 Ki = 4500.0 nM 5.35
CHEMBL4476596 Ki = 4800.0 nM 5.32
CHEMBL4572398 Ki = 4900.0 nM 5.31
CHEMBL4450287 Ki = 5220.0 nM 5.28
CHEMBL2408632 Ki = 5390.0 nM 5.27
CHEMBL4527223 Ki = 6540.0 nM 5.18
CHEMBL4585408 Ki = 8140.0 nM 5.09
CHEMBL4483357 Ki = 8200.0 nM 5.09
CHEMBL4592144 Ki = 8600.0 nM 5.07
CHEMBL4461148 Ki = 10750.0 nM 4.97
CHEMBL4461166 Ki = 10700.0 nM 4.97
CHEMBL4577468 Ki = 11890.0 nM 4.92
CHEMBL4531344 Ki = 12000.0 nM 4.92
CHEMBL4534257 Ki = 12120.0 nM 4.92
CHEMBL4574644 Ki = 13040.0 nM 4.88
CHEMBL4543944 Ki = 19000.0 nM 4.72
CHEMBL4527253 Ki = 18980.0 nM 4.72
CHEMBL4460750 Ki = 20050.0 nM 4.70
CHEMBL4467830 Ki = 20230.0 nM 4.69
CHEMBL4524803 Ki = 20500.0 nM 4.69
CHEMBL4530290 Ki = 23400.0 nM 4.63
CHEMBL4469452 Ki = 25700.0 nM 4.59
CHEMBL4443023 Ki = 26900.0 nM 4.57
CHEMBL4453213 Ki = 37700.0 nM 4.42
CHEMBL4592655 Ki = 40700.0 nM 4.39
CHEMBL4542552 Ki > 60000.0 nM -
CHEMBL4453600 Ki > 60000.0 nM -
CHEMBL4456729 Ki > 60000.0 nM -
CHEMBL4462458 Ki - -
CHEMBL4565611 Ki - -