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Assay Detail

CHEMBL5240233

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

ADMET
Inhibition of recombinant human CYP1B1 using 7-ethyl-0-resorufin as substrate incubated for 30 mins in presence of NADPH by EROD assay
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 1B1 (CHEMBL4878)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Drug Design and Synthesis of Novel <i>N</i>-Aryl-2,4-bithiazole-2-amine CYP1B1-Selective Inhibitors in Overcoming Taxol Resistance in A549 Cells.
Mao J, Wang D, Xu P, Wang Y, Zhang H, Wang S, Xu F, Wang J, Zhang F.
J Med Chem (2022) 65 : 16451 -16480
PubMed 36512763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 7.63 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5279681 1 10.05
CHEMBL5287897 1 9.26
CHEMBL5290149 1 8.92
CHEMBL5280516 1 8.75
CHEMBL5289888 1 8.41
CHEMBL5280415 1 8.30
CHEMBL5283668 1 8.22
CHEMBL5289447 1 8.20
CHEMBL5272094 1 8.19
CHEMBL5282966 1 8.18
CHEMBL5280088 1 8.18
CHEMBL5287228 1 8.15
CHEMBL5266178 1 8.13
CHEMBL5276078 1 8.12
CHEMBL5287748 1 8.10
CHEMBL46909 1 8.09
CHEMBL5269203 1 8.09
CHEMBL5273468 1 8.06
CHEMBL5278329 1 8.05
CHEMBL5290366 1 8.04
CHEMBL5282286 1 8.02
CHEMBL5288164 1 7.96
CHEMBL5268876 1 7.96
CHEMBL5268442 1 7.94
CHEMBL5280764 1 7.93
CHEMBL5276233 1 7.90
CHEMBL5278091 1 7.89
CHEMBL5276009 1 7.89
CHEMBL5268036 1 7.84
CHEMBL5290026 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5279681 IC50 = 0.09 nM 10.05
CHEMBL5287897 IC50 = 0.551 nM 9.26
CHEMBL5290149 IC50 = 1.21 nM 8.92
CHEMBL5280516 IC50 = 1.764 nM 8.75
CHEMBL5289888 IC50 = 3.915 nM 8.41
CHEMBL5280415 IC50 = 4.964 nM 8.30
CHEMBL5283668 IC50 = 6.062 nM 8.22
CHEMBL5289447 IC50 = 6.311 nM 8.20
CHEMBL5272094 IC50 = 6.494 nM 8.19
CHEMBL5282966 IC50 = 6.636 nM 8.18
CHEMBL5280088 IC50 = 6.6 nM 8.18
CHEMBL5287228 IC50 = 7.137 nM 8.15
CHEMBL5266178 IC50 = 7.452 nM 8.13
CHEMBL5276078 IC50 = 7.6 nM 8.12
CHEMBL5287748 IC50 = 7.875 nM 8.10
CHEMBL46909 IC50 = 8.225 nM 8.09
CHEMBL5269203 IC50 = 8.074 nM 8.09
CHEMBL5273468 IC50 = 8.672 nM 8.06
CHEMBL5278329 IC50 = 9.0 nM 8.05
CHEMBL5290366 IC50 = 9.093 nM 8.04
CHEMBL5282286 IC50 = 9.5 nM 8.02
CHEMBL5288164 IC50 = 11.06 nM 7.96
CHEMBL5268876 IC50 = 10.85 nM 7.96
CHEMBL5268442 IC50 = 11.58 nM 7.94
CHEMBL5280764 IC50 = 11.78 nM 7.93
CHEMBL5276233 IC50 = 12.72 nM 7.90
CHEMBL5276009 IC50 = 12.91 nM 7.89
CHEMBL5278091 IC50 = 12.91 nM 7.89
CHEMBL5268036 IC50 = 14.44 nM 7.84
CHEMBL5290026 IC50 = 15.85 nM 7.80
CHEMBL5290901 IC50 = 15.93 nM 7.80
CHEMBL5270385 IC50 = 16.7 nM 7.78
CHEMBL5281938 IC50 = 20.14 nM 7.70
CHEMBL5280421 IC50 = 22.19 nM 7.65
CHEMBL5270417 IC50 = 23.34 nM 7.63
CHEMBL5268929 IC50 = 26.82 nM 7.57
CHEMBL5267009 IC50 = 29.51 nM 7.53
CHEMBL5275398 IC50 = 33.14 nM 7.48
CHEMBL5279084 IC50 = 35.65 nM 7.45
CHEMBL5270072 IC50 = 39.02 nM 7.41
CHEMBL5276124 IC50 = 44.79 nM 7.35
CHEMBL5280700 IC50 = 51.28 nM 7.29
CHEMBL5272757 IC50 = 64.8 nM 7.19
CHEMBL5285319 IC50 = 65.1 nM 7.19
CHEMBL5275310 IC50 = 73.34 nM 7.13
CHEMBL5268347 IC50 = 76.81 nM 7.12
CHEMBL5270659 IC50 = 77.56 nM 7.11
CHEMBL5278510 IC50 = 86.24 nM 7.06
CHEMBL5276355 IC50 = 152.7 nM 6.82
CHEMBL5278641 IC50 = 156.16 nM 6.81