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Assay Detail

CHEMBL4019566

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

Binding
Inhibition of P-gp in human HCT116/VM46 cells assessed as reduction in cell viability after 72 hrs by phosphatase assay
184
Total Activities
184
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Vinblastine 20' Amides: Synthetic Analogues That Maintain or Improve Potency and Simultaneously Overcome Pgp-Derived Efflux and Resistance.
Lukesh JC, Carney DW, Dong H, Cross RM, Shukla V, Duncan KK, Yang S, Brody DM, Brütsch MM, Radakovic A, Boger DL.
J Med Chem (2017) 60 : 7591 -7604
PubMed 28857558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 184 7.34 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4090705 1 9.05
CHEMBL4076093 1 9.00
CHEMBL4082738 1 8.85
CHEMBL4069142 1 8.74
CHEMBL4062590 1 8.62
CHEMBL4094971 1 8.62
CHEMBL4090557 1 8.55
CHEMBL4088054 1 8.52
CHEMBL4092667 1 8.47
CHEMBL4071460 1 8.46
CHEMBL4081021 1 8.43
CHEMBL4092592 1 8.39
CHEMBL4059773 1 8.35
CHEMBL4068038 1 8.32
CHEMBL4081651 1 8.31
CHEMBL4090047 1 8.31
CHEMBL4099076 1 8.28
CHEMBL4099650 1 8.28
CHEMBL4060293 1 8.24
CHEMBL4102172 1 8.22
CHEMBL4104663 1 8.21
CHEMBL4088850 1 8.20
CHEMBL4068081 1 8.19
CHEMBL4064835 1 8.19
CHEMBL4087229 1 8.18
CHEMBL4096810 1 8.17
CHEMBL4103651 1 8.17
CHEMBL4068282 1 8.17
CHEMBL4085719 1 8.16
CHEMBL4070414 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4090705 IC50 = 0.9 nM 9.05
CHEMBL4076093 IC50 = 1.0 nM 9.00
CHEMBL4082738 IC50 = 1.4 nM 8.85
CHEMBL4069142 IC50 = 1.8 nM 8.74
CHEMBL4062590 IC50 = 2.4 nM 8.62
CHEMBL4094971 IC50 = 2.4 nM 8.62
CHEMBL4090557 IC50 = 2.8 nM 8.55
CHEMBL4088054 IC50 = 3.0 nM 8.52
CHEMBL4092667 IC50 = 3.4 nM 8.47
CHEMBL4071460 IC50 = 3.5 nM 8.46
CHEMBL4081021 IC50 = 3.7 nM 8.43
CHEMBL4092592 IC50 = 4.1 nM 8.39
CHEMBL4059773 IC50 = 4.5 nM 8.35
CHEMBL4068038 IC50 = 4.8 nM 8.32
CHEMBL4081651 IC50 = 4.9 nM 8.31
CHEMBL4090047 IC50 = 4.9 nM 8.31
CHEMBL4099076 IC50 = 5.2 nM 8.28
CHEMBL4099650 IC50 = 5.3 nM 8.28
CHEMBL4060293 IC50 = 5.7 nM 8.24
CHEMBL4102172 IC50 = 6.0 nM 8.22
CHEMBL4104663 IC50 = 6.2 nM 8.21
CHEMBL4088850 IC50 = 6.3 nM 8.20
CHEMBL4068081 IC50 = 6.4 nM 8.19
CHEMBL4064835 IC50 = 6.5 nM 8.19
CHEMBL4087229 IC50 = 6.6 nM 8.18
CHEMBL4103651 IC50 = 6.8 nM 8.17
CHEMBL4068282 IC50 = 6.7 nM 8.17
CHEMBL4096810 IC50 = 6.8 nM 8.17
CHEMBL4085719 IC50 = 6.9 nM 8.16
CHEMBL4070414 IC50 = 6.9 nM 8.16
CHEMBL4105494 IC50 = 7.3 nM 8.14
CHEMBL4073901 IC50 = 7.4 nM 8.13
CHEMBL4081777 IC50 = 7.6 nM 8.12
CHEMBL4088308 IC50 = 7.6 nM 8.12
CHEMBL4102710 IC50 = 7.5 nM 8.12
CHEMBL4074214 IC50 = 7.8 nM 8.11
CHEMBL4077516 IC50 = 7.7 nM 8.11
CHEMBL4089456 IC50 = 7.7 nM 8.11
CHEMBL4078959 IC50 = 8.0 nM 8.10
CHEMBL4069314 IC50 = 8.2 nM 8.09
CHEMBL4060924 IC50 = 8.4 nM 8.08
CHEMBL4091990 IC50 = 8.7 nM 8.06
CHEMBL4059860 IC50 = 8.7 nM 8.06
CHEMBL4090205 IC50 = 8.7 nM 8.06
CHEMBL4087285 IC50 = 8.9 nM 8.05
CHEMBL4079268 IC50 = 9.2 nM 8.04
CHEMBL4103227 IC50 = 9.2 nM 8.04
CHEMBL4102508 IC50 = 10.0 nM 8.00
CHEMBL4081719 IC50 = 11.0 nM 7.96
CHEMBL4099747 IC50 = 12.0 nM 7.92