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Assay Detail

CHEMBL2449559

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

Binding
SUPPLEMENTARY: Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay. Same assay as CHEMBL914418
ChEMBL ↗
303
Total Activities
303
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CCRF-CEM/VCR-1000
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

ATP-dependent translocase ABCB1 (CHEMBL4302) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity data for a series of P-glycoprotein inhibitors (Supplementary Data to CHEMBL1142990)
Ecker GF and Chiba P

· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 303 5.92 8.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2449435 — — 1 8.25
CHEMBL2449447 — — 1 7.89
CHEMBL2449394 — — 1 7.85
CHEMBL2449420 — — 1 7.77
CHEMBL2449498 — — 1 7.75
CHEMBL2449393 — — 1 7.74
CHEMBL2449392 — — 1 7.72
CHEMBL2449400 — — 1 7.59
CHEMBL2449344 — — 1 7.57
CHEMBL2449445 — — 1 7.51
CHEMBL2449466 — — 1 7.44
CHEMBL2449395 — — 1 7.42
CHEMBL2449454 — — 1 7.40
CHEMBL2449465 — — 1 7.35
CHEMBL2449483 — — 1 7.28
CHEMBL2449480 — — 1 7.25
CHEMBL2449354 — — 1 7.24
CHEMBL2449398 — — 1 7.23
CHEMBL2449516 — — 1 7.23
CHEMBL2449297 — — 1 7.15
CHEMBL2449346 — — 1 7.15
CHEMBL2449456 — — 1 7.13
CHEMBL2449408 — — 1 7.12
CHEMBL2449464 — — 1 7.10
CHEMBL2449496 — — 1 7.10
CHEMBL2449383 — — 1 7.09
CHEMBL2449467 — — 1 7.08
CHEMBL2449460 — — 1 7.07
CHEMBL389268 — — 1 7.01
CHEMBL2449376 — — 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2449435 — EC50 = 5.623 nM 8.25
CHEMBL2449447 — EC50 = 12.88 nM 7.89
CHEMBL2449394 — EC50 = 14.13 nM 7.85
CHEMBL2449420 — EC50 = 16.98 nM 7.77
CHEMBL2449498 — EC50 = 17.78 nM 7.75
CHEMBL2449393 — EC50 = 18.2 nM 7.74
CHEMBL2449392 — EC50 = 19.05 nM 7.72
CHEMBL2449400 — EC50 = 25.7 nM 7.59
CHEMBL2449344 — EC50 = 26.92 nM 7.57
CHEMBL2449445 — EC50 = 30.9 nM 7.51
CHEMBL2449466 — EC50 = 36.31 nM 7.44
CHEMBL2449395 — EC50 = 38.02 nM 7.42
CHEMBL2449454 — EC50 = 39.81 nM 7.40
CHEMBL2449465 — EC50 = 44.67 nM 7.35
CHEMBL2449483 — EC50 = 52.48 nM 7.28
CHEMBL2449480 — EC50 = 56.23 nM 7.25
CHEMBL2449354 — EC50 = 57.54 nM 7.24
CHEMBL2449398 — EC50 = 58.88 nM 7.23
CHEMBL2449516 — EC50 = 58.88 nM 7.23
CHEMBL2449297 — EC50 = 70.79 nM 7.15
CHEMBL2449346 — EC50 = 70.79 nM 7.15
CHEMBL2449456 — EC50 = 74.13 nM 7.13
CHEMBL2449408 — EC50 = 75.86 nM 7.12
CHEMBL2449496 — EC50 = 79.43 nM 7.10
CHEMBL2449464 — EC50 = 79.43 nM 7.10
CHEMBL2449383 — EC50 = 81.28 nM 7.09
CHEMBL2449467 — EC50 = 83.18 nM 7.08
CHEMBL2449460 — EC50 = 85.11 nM 7.07
CHEMBL389268 — EC50 = 97.72 nM 7.01
CHEMBL2449376 — EC50 = 109.65 nM 6.96
CHEMBL2449384 — EC50 = 114.82 nM 6.94
CHEMBL2449513 — EC50 = 114.82 nM 6.94
CHEMBL2449472 — EC50 = 120.23 nM 6.92
CHEMBL2449453 — EC50 = 125.89 nM 6.90
CHEMBL2449412 — EC50 = 128.82 nM 6.89
CHEMBL223130 — EC50 = 138.04 nM 6.86
CHEMBL2449288 — EC50 = 138.04 nM 6.86
CHEMBL2449425 — EC50 = 141.25 nM 6.85
CHEMBL2449419 — EC50 = 144.54 nM 6.84
CHEMBL2449515 — EC50 = 144.54 nM 6.84
CHEMBL2449389 — EC50 = 147.91 nM 6.83
CHEMBL2449296 — EC50 = 158.49 nM 6.80
CHEMBL2449452 — EC50 = 162.18 nM 6.79
CHEMBL2449426 — EC50 = 165.96 nM 6.78
CHEMBL2449471 — EC50 = 169.82 nM 6.77
CHEMBL2449377 — EC50 = 173.78 nM 6.76
CHEMBL2449503 — EC50 = 173.78 nM 6.76
CHEMBL2449356 — EC50 = 173.78 nM 6.76
CHEMBL2449369 — EC50 = 173.78 nM 6.76
CHEMBL2449358 — EC50 = 177.83 nM 6.75